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  1. Molecular and Immunological Mechanisms Underlying the Various Pharmacological Properties of the Potent Bioflavonoid, Rutin
    Yong DOC, Saker SR, Chellappan DK, Madheswaran T, Panneerselvam J, Choudhury H, et al.
    Endocr Metab Immune Disord Drug Targets, 2020;20(10):1590-1596.
    PMID: 32359343 DOI: 10.2174/1871530320666200503053846
    The application of medicinal plants has captured the interest of researchers in recent times due to their potent therapeutic properties and a better safety profile. The prominent role of herbal products in treating and preventing multiple diseases dates back to ancient history and most of the modern drugs today originated from their significant sources owing to their ability to control multiple targets via different signalling pathways. Among them, flavonoids consist of a large group of polyphenols, which are well known for their various therapeutic benefits. Rutin is considered one of the attractive phytochemicals and important flavonoids in the pharmaceutical industry due to its diverse pharmacological activities via various underlying molecular mechanisms. It is usually prescribed for various disease conditions such as varicosities, haemorrhoids and internal haemorrhage. In this review, we have discussed and highlighted the different molecular mechanisms attributed to the various pharmacological activities of rutin, such as antioxidant, anti-inflammatory, anticancer, anti-allergic and antidiabetic. This review will be beneficial to herbal, biological and molecular scientists in understanding the pharmacological relevance of rutin at the molecular level.
  2. Fulltext Tocotrienols-rich naringenin nanoemulgel for the management of diabetic wound: Fabrication, characterization and comparative in vitro evaluations
    Yeo E, Yew Chieng CJ, Choudhury H, Pandey M, Gorain B
    Curr Res Pharmacol Drug Discov, 2021;2:100019.
    PMID: 34909654 DOI: 10.1016/j.crphar.2021.100019
    The present research had been attempted to formulate and characterize tocotrienols-rich naringenin nanoemulgel for topical application in chronic wound conditions associated with diabetes. In due course, different phases of the nanoemulsion were chosen based on the solubility study, where combination of Capryol 90 and tocotrienols, Solutol HS15, and Transcutol P were selected as oil, surfactant, and cosurfactant, respectively. The nanoemulsions were formulated using the spontaneous emulsification method. Subsequently, Carbopols were incorporated to develop corresponding nanoemulgels of the optimized nanoemulsions. Thermodynamically stable optimized nanoemulgels were evaluated for their globule size, polydispersity index (PDI), surface charge, viscosity, mucoadhesive property, spreadability, in vitro release and release mechanism. Further, increasing polymer concentration in the nanoemulgels was reflected with the increased mucoadhesive property with corresponding decrease in the release rate of the drug. The optimized nanoemulgel (NG1) consisted of uniform dispersion (PDI, 0.452 ​± ​0.03) of the nanometric globules (145.58 ​± ​12.5) of the dispersed phase, and negative surface charge (-21.1 ​± ​3.32 ​mV) with viscosity 297,600 ​cP and good spreadability. In vitro release of naringenin in phosphate buffer saline revealed a sustained release profile up to a maximum of 74.62 ​± ​4.54% from the formulated nanoemulgel (NG1) within the time-frame of 24 ​h. Alternatively, the release from the nanoemulsion was much higher (89.17 ​± ​2.87%), which might be due to lack of polymer coating on the dispersed oil droplets. Moreover, the in vitro release kinetics from the nanoemulgel followed the first-order release and Higuchi model with non-Fickian diffusion. Therefore, encouraging results in this research is evident in bringing a promising future in wound management, particularly associated with diabetes complications.
  3. Fulltext Development of In-Situ Spray for Local Delivery of Antibacterial Drug for Hidradenitis Suppurativa: Investigation of Alternative Formulation
    Wong YL, Pandey M, Choudhury H, Lim WM, Bhattamisra SK, Gorain B
    Polymers (Basel), 2021 Aug 18;13(16).
    PMID: 34451309 DOI: 10.3390/polym13162770
    Hidradenitis suppurativa (HS) has been considered an orphan disease with limited treatments available. The available topical treatment for this condition is clindamycin lotion; however, short retention and frequent application are the main setbacks. Thus, the present study aimed to attain an optimized antibacterial in situ spray formulation for the hidradenitis suppurativa skin condition, which gels once in contact with the skin surface at around 37 °C and possesses bioadhesion as well as sustained-release properties of the incorporated drug. Different concentrations of thermo-reversible gelling polymer, Pluronic F-127, were investigated along with the selected bioadhesive polymers, HPMC and SA. The optimized formulation F3 consisting of 18% Pluronic F-127 with 0.2% HPMC and 0.2% SA was characterized based on various physicochemical properties. The gelation temperature of F3 was found to be 29.0 ± 0.50 °C with a gelation time of 1.35 ± 0.40 min and a pH of 5.8. F3 had the viscosity of 178.50 ± 5.50 cP at 25 °C and 7800 ± 200 cP at 37 °C as the gel set. The optimized formulation was found to be bioadhesive and cytocompatible. Cumulative drug release was 65.05% within the time-frame of 8 h; the release pattern of the drug followed zero-order kinetics with the Higuchi release mechanism. The average zone of inhibition was found to be 43.44 ± 1.34 mm. The properties of F3 formulation reflect to improve residence time at the site of application and can enhance sustained drug release. Therefore, it could be concluded that optimized formulation has better retention and enhanced antimicrobial activity for superior efficacy against HS.
  4. An insight into the role of Artificial Intelligence in the early diagnosis of Alzheimer's disease
    Verma RK, Pandey M, Chawla P, Choudhury H, Mayuren J, Bhattamisra SK, et al.
    CNS Neurol Disord Drug Targets, 2021 May 11.
    PMID: 33982657 DOI: 10.2174/1871527320666210512014505
    BACKGROUND: The complication of Alzheimer's disease (AD) has made the development of its therapeutic a challenging task. Even after decades of research, we have achieved no more than a few years of symptomatic relief. The inability to diagnose the disease early is the foremost hurdle behind its treatment. Several studies have aimed to identify potential biomarkers that can be detected in body fluids (CSF, blood, urine, etc) or assessed by neuroimaging (i.e., PET and MRI). However, the clinical implementation of these biomarkers is incomplete as they cannot be validated.

    METHOD: To overcome the limitation, the use of artificial intelligence along with technical tools has been extensively investigated for AD diagnosis. For developing a promising artificial intelligence strategy that can diagnose AD early, it is critical to supervise neuropsychological outcomes and imaging-based readouts with a proper clinical review.

    CONCLUSION: Profound knowledge, a large data pool, and detailed investigations are required for the successful implementation of this tool. This review will enlighten various aspects of early diagnosis of AD using artificial intelligence.

  5. Recent Advances in Self-Assembled Nanoparticles for Drug Delivery
    Varma LT, Singh N, Gorain B, Choudhury H, Tambuwala MM, Kesharwani P, et al.
    Curr Drug Deliv, 2020;17(4):279-291.
    PMID: 32039683 DOI: 10.2174/1567201817666200210122340
    The collection of different bulk materials forms the nanoparticles, where the properties of the nanoparticle are solely different from the individual components before being ensembled. Selfassembled nanoparticles are basically a group of complex functional units that are formed by gathering the individual bulk components of the system. It includes micelles, polymeric nanoparticle, carbon nanotubes, liposomes and niosomes, etc. This self-assembly has progressively heightened interest to control the final complex structure of the nanoparticle and its associated properties. The main challenge of formulating self-assembled nanoparticle is to improve the delivery system, bioavailability, enhance circulation time, confer molecular targeting, controlled release, protection of the incorporated drug from external environment and also serve as nanocarriers for macromolecules. Ultimately, these self-assembled nanoparticles facilitate to overcome the physiological barriers in vivo. Self-assembly is an equilibrium process where both individual and assembled components are subsisting in equilibrium. It is a bottom up approach in which molecules are assembled spontaneously, non-covalently into a stable and welldefined structure. There are different approaches that have been adopted in fabrication of self-assembled nanoparticles by the researchers. The current review is enriched with strategies for nanoparticle selfassembly, associated properties, and its application in therapy.
  6. Fulltext Dendrimer entrapped microsponge gel of dithranol for effective topical treatment
    Tripathi PK, Gorain B, Choudhury H, Srivastava A, Kesharwani P
    Heliyon, 2019 Mar;5(3):e01343.
    PMID: 30957038 DOI: 10.1016/j.heliyon.2019.e01343
    Dithranol is one of the important topical agents for the treatment of psoriasis, a chronic inflammatory skin disease with aberrant differentiation of keratinocytes. However, its application is troublesome and inconvenient because of its associated side effects, including staining, burning sensation, irritation, and necrotizing effect on the diseased cells as well as on the normal cells. The purpose of the current investigation was to explore the potential of poly(amido) amine (PAMAM) dendrimers in the topical delivery of dithranol through a novel microsponge based gel. Generation-4 (G4) dendrimers were incorporated into the microsponge based gel formulation by quasi-emulsion solvent diffusion method with varying concentration of polymers, and evaluated for the morphology of the formulation, encapsulation efficiency and skin irritation potential. Percentage yield of the formulation was found to be 66.28%, whereas encapsulation efficiency was ranged between 71.33% to 49.21%, and an average particle size was ranged between 28 ± 1.12 μm to 130 ± 1.01 μm. Surface morphology of developed microsponge was confirmed by scanning electron microscopy, revealed micro-porous nature. The optimized microsponge formulation was found to be stable and recorded non-irritant during cutaneous application of the experimental animals. Further, the pharmacokinetic outcomes of study were showed prolong penetration of the drug through the skin, equivalent to the marketed formulation of dithranol. Therefore, it could be conferred that the microsponge formulation of the PAMAM entrapped dithranol can produce prolonged efficacy without producing toxicities to the skin, and thus can effectively be projected in the treatment of diseases like psoriasis.
  7. Exploring the role of mesoporous silica nanoparticle in the development of novel drug delivery systems
    Stephen S, Gorain B, Choudhury H, Chatterjee B
    Drug Deliv Transl Res, 2022 Jan;12(1):105-123.
    PMID: 33604837 DOI: 10.1007/s13346-021-00935-4
    The biocompatible nature of mesoporous silica nanoparticles (MSN) attracted researchers' attention to deliver therapeutic agents in the treatment of various diseases, where their porous nature, high drug loading efficiency, and suitability to functionalize with a specific ligand of MSN helped to obtain the desired outcome. The application of MSN has been extended to deliver small chemicals to large-sized peptides or proteins to fight against complex diseases. Recently, formulation researches with MSN have been progressed for various non-conventional drug delivery systems, including liposome, microsphere, oro-dispersible film, 3D-printed formulation, and microneedle. Low bulk density, retaining mesoporous structure during downstream processing, and lack of sufficient in vivo studies are some of the important issues towards the success of mesoporous silica-based advanced drug delivery systems. The present review has aimed to evaluate the application of MSN in advanced drug delivery systems to critically analyze the role of MSN in the respective formulation over other functionalized polymers. Finally, an outlook on the future direction of MSN-based advanced drug delivery systems has been drawn against the existing challenges with this platform.
  8. Pharmacokinetics and tissue distribution of hydrazinocurcumin in rats
    Satyavert, Gupta S, Choudhury H, Jacob S, Nair AB, Dhanawat M, et al.
    Pharmacol Rep, 2021 Dec;73(6):1734-1743.
    PMID: 34283375 DOI: 10.1007/s43440-021-00312-5
    BACKGROUND: Curcumin, a natural polyphenol from Curcuma longa, is known to possess diversified pharmacological roles including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic properties; however, its bioavailability is severely limited due to its poor solubility, poor absorption, rapid metabolism, and significant elimination. Hydrazinocurcumin (HZC), a novel analogue of curcumin has been reported to overcome the limitations of curcumin and also possesses multiple pharmacological activities. The present study aimed to evaluate the unexplored pharmacokinetic profile of this agent in experimental rats.

    METHODS: Drug formulations were administered to the experimental animals via oral, intravenous and intraperitoneal routes. Blood samples were collected at different pre-determined time intervals to determine the pharmacokinetic parameters. To understand the biodistribution profile of HCZ, tissue samples were isolated from different groups of Sprague-Dawley rats at different time points. The pharmacokinetic parameters of HZC were evaluated after administration through oral (100 mg/kg), intraperitoneal (100 mg/kg) and intravenous (10 mg/kg) routes.

    RESULTS: Significantly (p 

  9. Recent update of toxicity aspects of nanoparticulate systems for drug delivery
    Patnaik S, Gorain B, Padhi S, Choudhury H, Gabr GA, Md S, et al.
    Eur J Pharm Biopharm, 2021 Apr;161:100-119.
    PMID: 33639254 DOI: 10.1016/j.ejpb.2021.02.010
    Potential research outcomes on nanotechnology-based novel drug delivery systems since the past few decades attracted the attention of the researchers to overcome the limitations of conventional deliveries. Apart from possessing enhanced solubility of poorly water-soluble drugs, the targeting potential of the carriers facilitates longer circulation and site-specific delivery of the entrapped therapeutics. The practice of these delivery systems, therefore, helps in maximizing bioavailability, improving pharmacokinetics profile, pharmacodynamics activity and biodistribution of the entrapped drug(s). In addition to focusing on the positive side, evaluation of nanoparticulate systems for toxicity is a crucial parameter for its biomedical applications. Due to the size of nanoparticles, they easily traverse through biological barriers and may be accumulated in the body, where the ingredients incorporated in the formulation development might accumulate and/or produce toxic manifestation, leading to cause severe health hazards. Therefore, the toxic profile of these delivery systems needs to be evaluated at the molecular, cellular, tissue and organ level. This review offers a comprehensive presentation of toxicity aspects of the constituents of nanoparticular based drug delivery systems, which would be beneficial for future researchers to develop nanoparticulate delivery vehicles for the improvement of delivery approaches in a safer way.
  10. Fulltext Budesonide-Loaded Pectin/Polyacrylamide Hydrogel for Sustained Delivery: Fabrication, Characterization and In Vitro Release Kinetics
    Pandey M, Choudhury H, D/O Segar Singh SK, Chetty Annan N, Bhattamisra SK, Gorain B, et al.
    Molecules, 2021 May 05;26(9).
    PMID: 34062995 DOI: 10.3390/molecules26092704
    A single ulcerative colitis (UC) is a chronic inflammatory bowel disease (IBD) that causes inflammation of the colonic mucosa at the distal colon and rectum. The mainstay therapy involves anti-inflammatory immunosuppression based on the disease location and severity. The disadvantages of using systemic corticosteroids for UC treatment is the amplified risk of malignancies and infections. Therefore, topical treatments are safer as they have fewer systemic side effects due to less systemic exposure. In this context, pH sensitive and enzymatically triggered hydrogel of pectin (PC) and polyacrylamide (PAM) has been developed to facilitate colon-targeted delivery of budesonide (BUD) for the treatment of UC. The hydrogels were characterized by Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), swelling ratio, and drug release. FT-IR spectroscopy confirmed the grafting as well loading of BUD in hydrogel. XRD showed the amorphous nature of hydrogel and increment in crystallinity after drug loading. On the other hand, SEM showed that the hydrogels exhibited a highly porous morphology, which is suitable for drug loading and also demonstrated a pH-responsive swelling behaviour, with decreased swelling in acidic media. The in-vitro release of BUD from the hydrogel exhibited a sustained release behaviour with non-ficken diffusion mechanism. The model that fitted best for BUD released was the Higuchi kinetic model. It was concluded that enzyme/pH dual-sensitive hydrogels are an effective colon-targeted delivery system for UC.
  11. 3D printing for oral drug delivery: a new tool to customize drug delivery
    Pandey M, Choudhury H, Fern JLC, Kee ATK, Kou J, Jing JLJ, et al.
    Drug Deliv Transl Res, 2020 08;10(4):986-1001.
    PMID: 32207070 DOI: 10.1007/s13346-020-00737-0
    The involvement of recent technologies, such as nanotechnology and three-dimensional printing (3DP), in drug delivery has become the utmost importance for effective and safe delivery of potent therapeutics, and thus, recent advancement for oral drug delivery through 3DP technology has been expanded. The use of computer-aided design (CAD) in 3DP technology allows the manufacturing of drug formulation with the desired release rate and pattern. Currently, the most applicable 3DP technologies in the oral drug delivery system are inkjet printing method, fused deposition method, nozzle-based extrusion system, and stereolithographic 3DP. In 2015, the first 3D-printed tablet was approved by the US Food and Drug Administration (FDA), and since then, it has opened up more opportunities in the discovery of formulation for the development of an oral drug delivery system. 3DP allows the production of an oral drug delivery device that enables tailor-made formulation with customizable size, shape, and release rate. Despite the advantages offered by 3DP technology in the drug delivery system, there are challenges in terms of drug stability, safety as well as applicability in the clinical sector. Nonetheless, 3DP has immense potential in the development of drug delivery devices for future personalized medicine. This article will give the recent advancement along with the challenges of 3DP techniques for the development of oral drug delivery. Graphical abstract.
  12. Recent Updates on Novel Approaches in Insulin Drug Delivery: A Review of Challenges and Pharmaceutical Implications
    Pandey M, Choudhury H, Yi CX, Mun CW, Phing GK, Rou GX, et al.
    Curr Drug Targets, 2018;19(15):1782-1800.
    PMID: 29792143 DOI: 10.2174/1389450119666180523092100
    Diabetes mellitus, a metabolic disorder of glucose metabolism, is mainly associated with insulin resistance to the body cells, or impaired production of insulin by the pancreatic β-cells. Insulin is mainly required to regulate glucose metabolism in type 1 diabetes mellitus patients; however, many patients with type 2 diabetes mellitus also require insulin, especially when their condition cannot be controlled solely by oral hypoglycemic agents. Hence, major research is ongoing attempting to improve the delivery of insulin in order to make it more convenient to patients who experience side effects from the conventional treatment procedure or non-adherence to insulin regimen due to multiple comorbid conditions. Conventionally, insulin is administered via subcutaneous route which is also one of the sole reasons of patient's non-compliance due to the invasiveness of this method. Several attempts have been done to improve patient compliance, reduce side effects, improve delivery adherence, and to enhance the pharmaceutical performance of the insulin therapy. Despite facing substantial challenges in developing efficient delivery systems for insulin, vast research studies have been carried out for the development of smart delivery systems to deliver insulin via ocular, buccal, pulmonary, oral, transdermal, as well as rectal routes. Therefore, the present review was aimed to overview the challenges encountered with the current insulin delivery systems and to summarize recent advancements in technology of various novel insulin delivery systems being discovered and introduced in the current market.
  13. Perspectives of Nanoemulsion Strategies in The Improvement of Oral, Parenteral and Transdermal Chemotherapy
    Pandey M, Choudhury H, Yeun OC, Yin HM, Lynn TW, Tine CLY, et al.
    Curr Pharm Biotechnol, 2018;19(4):276-292.
    PMID: 29874994 DOI: 10.2174/1389201019666180605125234
    BACKGROUND: Targeting chemotherapeutic agents to the tumor tissues and achieving accumulation with ideal release behavior for desired therapy requires an ideal treatment strategy to inhibit division of rapid growing cancerous cells and as an outcome improve patient's quality of life. However, majority of the available anticancer therapies are well known for their systemic toxicities and multidrug resistance.

    METHODS: Application of nanotechnology in medicine have perceived a great evolution during past few decades. Nanoemulsion, submicron sized thermodynamically stable distribution of two immiscible liquids, has gained extensive importance as a nanocarrier to improve chemotherapies seeking to overcome the limitations of drug solubilization, improving systemic delivery of the chemotherapeutics to the site of action to achieve a promising inhibitory in tumor growth profile with reduced systemic toxicity.

    RESULTS AND CONCLUSION: This review has focused on potential application of nanoemulsion in the translational research and its role in chemotherapy using oral, parenteral and transdermal route to enhance systemic availability of poorly soluble drug. In summary, nanoemulsion is a multifunctional nanocarrier capable of enhancing drug delivery potential of cytotoxic agents, thereby, can improve the outcomes of cancer treatment by increasing the life-span of the patient and quality of life, however, further clinical research and characterization of interactive reactions should need to be explored.

  14. Nanoparticles Based Intranasal Delivery of Drug to Treat Alzheimer's Disease: A Recent Update
    Pandey M, Choudhury H, Verma RK, Chawla V, Bhattamisra SK, Gorain B, et al.
    CNS Neurol Disord Drug Targets, 2020;19(9):648-662.
    PMID: 32819251 DOI: 10.2174/1871527319999200819095620
    Alzheimer Association Report (2019) stated that the 6th primary cause of death in the USA is Alzheimer's Disease (AD), which leads to behaviour and cognitive impairment. Nearly 5.8 million peoples of all ages in the USA have suffered from this disease, including 5.6 million elderly populations. The statistics of the progression of this disease is similar to the global scenario. Still, the treatment of AD is limited to a few conventional oral drugs, which often fail to deliver an adequate amount of the drug in the brain. The reduction in the therapeutic efficacy of an anti-AD drug is due to poor solubility, existence to the blood-brain barrier and low permeability. In this context, nasal drug delivery emerges as a promising route for the delivery of large and small molecular drugs for the treatment of AD. This promising pathway delivers the drug directly into the brain via an olfactory route, which leads to the low systemic side effect, enhanced bioavailability, and higher therapeutic efficacy. However, few setbacks, such as mucociliary clearance and poor drug mucosal permeation, limit its translation from the laboratory to the clinic. The above stated limitation could be overcome by the adaption of nanoparticle as a drug delivery carrier, which may lead to prolong delivery of drugs with better permeability and high efficacy. This review highlights the latest work on the development of promising Nanoparticles (NPs) via the intranasal route for the treatment of AD. Additionally, the current update in this article will draw the attention of the researcher working on these fields and facing challenges in practical applicability.
  15. Fulltext Site-Specific Vesicular Drug Delivery System for Skin Cancer: A Novel Approach for Targeting
    Pandey M, Choudhury H, Gorain B, Tiong SQ, Wong GYS, Chan KX, et al.
    Gels, 2021 Nov 16;7(4).
    PMID: 34842689 DOI: 10.3390/gels7040218
    Skin cancer, one of the most prevalent cancers worldwide, has demonstrated an alarming increase in prevalence and mortality. Hence, it is a public health issue and a high burden of disease, contributing to the economic burden in its treatment. There are multiple treatment options available for skin cancer, ranging from chemotherapy to surgery. However, these conventional treatment modalities possess several limitations, urging the need for the development of an effective and safe treatment for skin cancer that could provide targeted drug delivery and site-specific tumor penetration and minimize unwanted systemic toxicity. Therefore, it is vital to understand the critical biological barriers involved in skin cancer therapeutics for the optimal development of the formulations. Various nanocarriers for targeted delivery of chemotherapeutic drugs have been developed and extensively studied to overcome the limitations faced by topical conventional dosage forms. A site-specific vesicular drug delivery system appears to be an attractive strategy in topical drug delivery for the treatment of skin malignancies. In this review, vesicular drug delivery systems, including liposomes, niosomes, ethosomes, and transfersomes in developing novel drug delivery for skin cancer therapeutics, are discussed. Firstly, the prevalence statistics, current treatments, and limitations of convention dosage form for skin cancer treatment are discussed. Then, the common type of nanocarriers involved in the research for skin cancer treatment are summarized. Lastly, the utilization of vesicular drug delivery systems in delivering chemotherapeutics is reviewed and discussed, along with their beneficial aspects over other nanocarriers, safety concerns, and clinical aspects against skin cancer treatment.
  16. Hyaluronic acid-modified betamethasone encapsulated polymeric nanoparticles: fabrication, characterisation, in vitro release kinetics, and dermal targeting
    Pandey M, Choudhury H, Gunasegaran TAP, Nathan SS, Md S, Gorain B, et al.
    Drug Deliv Transl Res, 2019 04;9(2):520-533.
    PMID: 29488170 DOI: 10.1007/s13346-018-0480-1
    Atopic dermatitis (AD) is a chronically relapsing eczematous skin disease characterised by frequent episodes of rashes, severe flares, and inflammation. Till date, there is no absolute therapy for the treatment of AD; however, topical corticosteroids (TCs) are the majorly prescribed class of drugs for the management of AD in both adults and children. Though, topical route is most preferable; however, limited penetration of therapeutics across the startum cornum (SC) is one of the major challenges for scientists. Therefore, the present study was attempted to fabricate a moderate-potency TC, betamethasone valerate (BMV), in the form of chitosan nanoparticles (CS-NPs) for optimum dermal targeting and improved penetration across the SC. To further improve the targeting efficiency of BMV and to potentiate its therapeutic efficacy, the fabricated BMV-CS-NPs were coated with hyaluronic acid (HA). The prepared NPs were characterised for particle size, zeta potential, polydispersity index (PDI), entrapment efficiency, loading capacity, crystallinity, thermal behaviour, morphology, in vitro release kinetics, drug permeation across the SC, and percentage of drug retained into various skin layers. Results showed that optimised HA-BMV-CS-NPs exhibited optimum physicochemical characteristics including finest particle size (
  17. Fulltext Potential of Stimuli-Responsive In Situ Gel System for Sustained Ocular Drug Delivery: Recent Progress and Contemporary Research
    Pandey M, Choudhury H, Binti Abd Aziz A, Bhattamisra SK, Gorain B, Su JST, et al.
    Polymers (Basel), 2021 Apr 20;13(8).
    PMID: 33923900 DOI: 10.3390/polym13081340
    Eyesight is one of the most well-deserved blessings, amid all the five senses in the human body. It captures the raw signals from the outside world to create detailed visual images, granting the ability to witness and gain knowledge about the world. Eyes are exposed directly to the external environment; they are susceptible to the vicissitudes of diseases. The World Health Organization has predicted that the number of individuals affected by eye diseases will rise enormously in the next decades. However, the physical barriers of the eyes and the problems associated with conventional ocular formulations are significant challenges in ophthalmic drug development. This has generated the demand for a sustained ocular drug delivery system, which serves to deliver effective drug concentration at a reduced frequency for consistent therapeutic effect and better patient treatment adherence. Recent advancement in pharmaceutical dosage design has demonstrated that a stimuli-responsive in situ gel system exhibits the favorable characteristics for providing sustained ocular drug delivery and enhanced ocular bioavailability. Stimuli-responsive in situ gels undergo a phase transition (solution-gelation) in response to the ocular environmental temperature, pH, and ions. These stimuli transform the formulation into a gel at the cul de sac to overcome the shortcomings of conventional eye drops, such as rapid nasolacrimal drainage and short contact time with the ocular surface This review highlights the recent successful research outcomes of stimuli-responsive in situ gelling systems in treating in vivo models with glaucoma and various ocular infections. Additionally, it also presents the mechanism, recent development, and safety considerations of stimuli-sensitive in situ gel as the potential sustained ocular delivery system for treating common eye disorders.
  18. In vitro neuroprotective effects of naringenin nanoemulsion against β-amyloid toxicity through the regulation of amyloidogenesis and tau phosphorylation
    Md S, Gan SY, Haw YH, Ho CL, Wong S, Choudhury H
    Int J Biol Macromol, 2018 Oct 15;118(Pt A):1211-1219.
    PMID: 30001606 DOI: 10.1016/j.ijbiomac.2018.06.190
    Alzheimer's disease (AD) is an increasingly prevalent neurological disorder of the central nervous system. There is growing evidence that amyloidogenesis is a pathological hallmark for AD; this leads to the formation of senile plaques. Naringenin is a bioflavonoid which has neuroprotective effects through its antioxidant and anti-inflammatory properties. However, its clinical usage is limited due to its inefficient transport across biological membranes. In the present study, a naringenin nanoemulsion was prepared and its neuroprotective effects were tested against β-amyloid induced neurotoxicity in a human neuroblastoma cell line (SH-SY5Y). The optimised, naringenin-loaded nanoemulsion formulation had a droplet size of 113.83 ± 3.35 nm and around 50 nm, as assessed respectively by photon correlation spectroscopy and transmission electron microscopy. The preparation showed a low polydispersity index (0.312 ± 0.003), a high zeta potential (12.4 ± 1.05) and a high percentage transmittance (97.01%). The neuroprotective activity of naringenin nanoemulsions was determined by assessing their ability to protect SH-SY5Y neuroblastoma cells against the neurotoxic effect of beta amyloid (Aβ). Aβ-induced production of reactive oxygen species (ROS), amyloid precursor protein (APP), β-secretase (BACE), total tau and phosphorylated tau (pT231) was also determined. The naringenin loaded nanoemulsion significantly alleviated the direct neurotoxic effects of Aβ on SH-SY5Y cells; this was associated with a down-regulation of APP and BACE expression, indicating reduced amyloidogenesis. Furthermore, it decreased the levels of phosphorylated tau in SH-SY5Y cells exposed to Aβ. These results suggest that a naringenin-loaded nanoemulsion could be a promising agent for the treatment of Alzheimer's disease.
  19. Nanoencapsulation of betamethasone valerate using high pressure homogenization-solvent evaporation technique: optimization of formulation and process parameters for efficient dermal targeting
    Md S, Kuldeep Singh JKA, Waqas M, Pandey M, Choudhury H, Habib H, et al.
    Drug Dev Ind Pharm, 2019 Feb;45(2):323-332.
    PMID: 30404554 DOI: 10.1080/03639045.2018.1542704
    Betamethsone valerate (BMV), a medium potency topical corticosteroid, is one of the most commonly employed pharmacological agents for the management of atopic dermatitis in both adults and children. Despite having remarkable pharmacological efficacy, these agents have limited clinical implication due to poor penetration across the startum cornum (SC). To mitigate issues related to targeted delivery, stability, and solubility as well as to potentiate therapeutic and clinical implication, the nanodelivery systems have gained remarkable recognition. Therefore, this study was aimed to encapsulate BMV into the chitosan nanoparticles (CS-NPs) for optimum dermal targeting and improved penetration across the SC. The prepared NPs were characterized for particle size, zeta potential, polydispersity index, entrapment efficiency, loading capacity, crystallinity, thermal behavior, morphology, in vitro release kinetics, drug permeation across the SC, and percentage of drug retained into various skin layers. Results showed that optimized BMV-CS-NPs exhibited optimum physicochemical characteristics including small particle size (< 250 ± 28 nm), higher zeta potential (+58 ± 8 mV), and high entrapment efficiency (86 ± 5.6%) and loading capacity (34 ± 7.2%). The in vitro release study revealed that BMV-CS-NPs displayed Fickian-diffusion type mechanism of release in simulated skin surface (pH 5.5). Drug permeation efficiency and the amount of BMV retained into the epidermis and the dermis were comparatively higher in case of BMV-CS-NPs compared to BMV solution. Conclusively, we anticipated that BMV-CS-NPs could be a promising nanodelivery system for efficient dermal targeting of BMV and improved anti-AD efficacy.
  20. Antipsychotic Potential and Safety Profile of TPGS-Based Mucoadhesive Aripiprazole Nanoemulsion: Development and Optimization for Nose-To-Brain Delivery
    Kumbhar SA, Kokare CR, Shrivastava B, Gorain B, Choudhury H
    J Pharm Sci, 2021 04;110(4):1761-1778.
    PMID: 33515583 DOI: 10.1016/j.xphs.2021.01.021
    Delivering therapeutics to the brain using conventional dosage forms is always a challenge, thus the present study was aimed to formulate mucoadhesive nanoemulsion (MNE) of aripiprazole (ARP) for intranasal delivery to transport the drug directly to the brain. Therefore, a TPGS based ARP-MNE was formulated and optimized using the Box-Behnken statistical design. The improved in vitro release profile of the formulation was in agreement to enhanced ex vivo permeation through sheep mucous membranes with a maximum rate of permeation co-efficient (62.87  cm h-1 × 103) and flux (31.43  μg cm-2.h-1). The pharmacokinetic profile following single-dose administration showed the maximum concentration of drug in the brain (Cmax) of 15.19 ± 2.51  μg mL-1 and Tmax of 1 h in animals with ARP-MNE as compared to 10.57 ± 1.88  μg mL-1 and 1 h, and 2.52 ± 0.38  μg mL-1 and 3 h upon intranasal and intravenous administration of ARP-NE, respectively. Further, higher values of % drug targeting efficiency (96.9%) and % drug targeting potential (89.73%) of ARP-MNE through intranasal administration were investigated. The studies in Wistar rats showed no existence of extrapyramidal symptoms through the catalepsy test and forelimb retraction results. No ex vivo ciliotoxicity on nasal mucosa reflects the safety of the components and delivery tool. Further, findings on locomotor activity and hind-limb retraction test in ARP-MNE treated animals established its antipsychotic efficacy. Thus, it can be inferred that the developed ARP-MNE could effectively be explored as brain delivery cargo in the effective treatment of schizophrenia without producing any toxic manifestation.
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