Displaying publications 61 - 80 of 511 in total

Abstract:
Sort:
  1. Rasool M, Malik A, Waquar S, Arooj M, Zahid S, Asif M, et al.
    Bioengineered, 2022 Jan;13(1):759-773.
    PMID: 34856849 DOI: 10.1080/21655979.2021.2012907
    Nanomedicines are applied as alternative treatments for anticancer agents. For the treatment of cancer, due to the small size in nanometers (nm), specific site targeting can be achieved with the use of nanomedicines, increasing their bioavailability and conferring fewer toxic side effects. Additionally, the use of minute amounts of drugs can lead to cost savings. In addition, nanotechnology is effectively applied in the preparation of such drugs as they are in nm sizes, considered one of the earliest cutoff values for the production of products utilized in nanotechnology. Early concepts described gold nanoshells as one of the successful therapies for cancer and associated diseases where the benefits of nanomedicine include effective active or passive targeting. Common medicines are degraded at a higher rate, whereas the degradation of macromolecules is time-consuming. All of the discussed properties are responsible for executing the physiological behaviors occurring at the following scale, depending on the geometry. Finally, large nanomaterials based on organic, lipid, inorganic, protein, and synthetic polymers have also been utilized to develop novel cancer cures.
    Matched MeSH terms: Drug Delivery Systems
  2. Ali A, Akhtar J, Ahmad U, Basheer AS, Jaiswal N, Jahan A
    PMID: 36374840 DOI: 10.1615/CritRevTherDrugCarrierSyst.2022039241
    Colorectal cancer (CRC) is the second most common cause of cancer related deaths in the United States. However, more than half of all incidence and mortality are caused by risk factors such as smoking, unhealthy diet, excessive alcohol consumption, inactivity, and excess weight, and thus can be protected. CRC morbidity and mortality can also be reduced by proper screening and monitoring. Over the last few years the amalgamation of nanotechnology with healthcare system has brought about the potential to administer the delivery of certain therapeutic drugs to cancer cells without affecting normal tissues. Recent strategies combine the diagnostic and therapeutic approaches to improve the overall performance of cancer nanomedicines. Targeted cancer nanotherapeutics provides many more opportunities for the selective detection of toxic chemicals within cancer cells. The distinctive features of nanoparticles, such as their small size, large surface to volume ratio, and the ability of nanoparticles to achieve several interactions of ligands at surface, offer great benefits of nanomedicines to treat various types of cancers. This review highlights the molecular mechanisms of colorectal carcinogenesis and discusses various key concepts in the development of nanotherapeutics targeted for CRC treatment.
    Matched MeSH terms: Drug Delivery Systems
  3. Shukla MK, Dubey A, Pandey S, Singh SK, Gupta G, Prasher P, et al.
    Curr Pharm Des, 2022;28(39):3202-3211.
    PMID: 35422206 DOI: 10.2174/1381612828666220413103831
    Several factors exist that limit the efficacy of lung cancer treatment. These may be tumor-specific delivery of therapeutics, airway geometry, humidity, clearance mechanisms, presence of lung diseases, and therapy against tumor cell resistance. Advancements in drug delivery using nanotechnology based multifunctional nanocarriers, have emerged as a viable method for treating lung cancer with more efficacy and fewer adverse effects. This review does a thorough and critical examination of effective nano-enabled approaches for lung cancer treatment, such as nano-assisted drug delivery systems. In addition, to therapeutic effectiveness, researchers have been working to determine several strategies to produce nanotherapeutics by adjusting the size, drug loading, transport, and retention. Personalized lung tumor therapies using sophisticated nano modalities have the potential to provide great therapeutic advantages based on individual unique genetic markers and disease profiles. Overall, this review provides comprehensive information on newer nanotechnological prospects for improving the management of apoptosis in lung cancer.
    Matched MeSH terms: Drug Delivery Systems/methods
  4. Woon CK, Hui WK, Abas R, Haron MH, Das S, Lin TS
    Curr Neuropharmacol, 2022;20(8):1498-1518.
    PMID: 34923947 DOI: 10.2174/1570159X20666211217163540
    Alzheimer's disease (AD) affects the elderly and is characterized by progressive neurodegeneration caused by different pathologies. The most significant challenges in treating AD include the inability of medications to reach the brain because of its poor solubility, low bioavailability, and the presence of the blood-brain barrier (BBB). Additionally, current evidence suggests the disruption of BBB plays an important role in the pathogenesis of AD. One of the critical challenges in treating AD is the ineffective treatments and their severe adverse effects. Nanotechnology offers an alternative approach to facilitate the treatment of AD by overcoming the challenges in drug transport across the BBB. Various nanoparticles (NP) loaded with natural products were reported to aid in drug delivery for the treatment of AD. The nano-sized entities of NP are great platforms for incorporating active materials from natural products into formulations that can be delivered effectively to the intended action site without compromising the material's bioactivity. The review highlights the applications of medicinal plants, their derived components, and various nanomedicinebased approaches for the treatment of AD. The combination of medicinal plants and nanotechnology may lead to new theragnostic solutions for the treatment of AD in the future.
    Matched MeSH terms: Drug Delivery Systems
  5. Antonov II, Dymnikov AB, Muraev AA, Ananyeva LA, Ivanov SY
    Sovrem Tekhnologii Med, 2022;14(4):43-48.
    PMID: 37179985 DOI: 10.17691/stm2022.14.4.05
    The aim of the study was to evaluate the use of barophoresis for the delivery of liquid-air drug substances to the gums using a mathematical model of the interaction of the drug mixture with periodontal tissues.

    MATERIALS AND METHODS: The solution to the problem was preceded by generation of a geometric CAD model of the device and nozzle for barophoresis, including the nozzle and injector geometry. The Ansys SpaceClaim software package was used to generate the CAD geometry.

    RESULTS: When solving the problem of finding the optimal distance from the nozzle to the gum surface, the numerical modeling showed that at a distance of 5 mm, the volume fraction of liquid in the mixture is 18-20%. The mixture actually breaks through the gum, filling 0.8 mm of the gum thickness and spreading symmetrically to the sides at a distance of up to 3 cm, forming a cavity. At a distance of 10 mm from the nozzle to the gum surface, the liquid volume fraction in the mixture close to the gum lies in a narrow range of values of 5 to 7%. The mixture touches the surface of the gums, penetrating slightly - at a distance of 0.30-0.45 mm. At a distance of 15 mm from the nozzle to the gum surface, the volume fraction of liquid in the mixture near the gum lies in the range of 2-5%. The mixture slightly touches the gum surface, getting inside at a distance of up to 0.2 mm, having practically no effect on the gum.

    CONCLUSION: The developed mathematical model confirmed the feasibility of application of barophoresis in the treatment of chronic generalized periodontitis. The optimal distance from the nozzle to the surface should be considered to be 10-15 mm. This distance is safe and allows the drug delivery to a depth of 0.45 mm.

    Matched MeSH terms: Drug Delivery Systems*
  6. Zhang W, Lv Z, Zhang Y, Gopinath SCB, Yuan Y, Huang D, et al.
    Oxid Med Cell Longev, 2022;2022:6006601.
    PMID: 36211824 DOI: 10.1155/2022/6006601
    OBJECTIVE: The off-target effects and severe side effects of PPARα and LXRα agonists greatly limit their application in atherosclerosis (AS). Therefore, this study intended to use mesoporous silica nanoparticles as carriers to generate MnO nanoparticles in situ with T1WI-MRI in mesoporous pores and simultaneously load PPARα and LXRα agonists. Afterward, cRGD-chelated platelet membranes can be used for coating to construct a new nanotheranostic agent.

    METHODS: cRGD-platelet@MnO/MSN@PPARα/LXRα nanoparticles were synthesized by a chemical method. Dynamic light scattering (DLS) was utilized to detect the size distribution and polydispersity index (PDI) of the nanoparticles. The safety of the nanoparticles was detected by CCK8 in vitro and HE staining and kidney function in vivo. Cell apoptosis was detected by flow cytometry detection and TUNEL staining. Oxidative stress responses (ROS, SOD, MDA, and NOX levels) were tested via a DCFH-DA assay and commercial kits. Immunofluorescence and phagocytosis experiments were used to detect the targeting of nanoparticles. Magnetic resonance imaging (MRI) was used to detect the imaging performance of cRGD-platelet@MnO/MSN@PPARα/LXRα nanoparticles. Using western blotting, the expression changes in LXRα and ABCA1 were identified.

    RESULTS: cRGD-platelet@MnO/MSN@PPARα/LXRα nanoparticles were successfully established, with a particle size of approximately 150 nm and PDI less than 0.3, and showed high safety both in vitro and in vivo. cRGD-platelet@MnO/MSN@PPARα/LXRα nanoparticles showed good targeting properties and better MRI imaging performance in AS. cRGD-platelet@MnO/MSN@PPARα/LXRα nanoparticles showed better antioxidative capacities, MRI imaging performance, and diagnostic and therapeutic effects on AS by regulating the expression of LXRα and ABCA1.

    CONCLUSION: In the present study, cRGD-platelet@MnO/MSN@PPARα/LXRα nanoparticles with high safety and the capacity to target vulnerable plaques of AS were successfully established. They showed better performance on MRI images and treatment effects on AS by promoting cholesterol efflux through the regulation of ABCA1. These findings might address the problems of off-target effects and side effects of nanoparticle-mediated drug delivery, which will enhance the efficiency of AS treatment and provide new ideas for the clinical treatment of AS.

    Matched MeSH terms: Drug Delivery Systems
  7. Samrot AV, Saigeetha S, Mun CY, Abirami S, Purohit K, Cypriyana PJJ, et al.
    Sci Rep, 2021 12 31;11(1):24511.
    PMID: 34972829 DOI: 10.1038/s41598-021-03328-2
    Latex, a milky substance found in a variety of plants which is a natural source of biologically active compounds. In this study, Latex was collected from raw Carica papaya and was characterized using UV-Vis, FTIR and GC-MS analyses. Super Paramagnetic Iron Oxide Nanoparticles (SPIONs) were synthesized, coated with C. papaya latex (PL-Sp) and characterized using UV-Vis, FT-IR, SEM-EDX, XRD, VSM and Zeta potential analyses. SPIONs and latex coated SPIONs (PL-Sp) were used in batch adsorption study for effective removal of Methylene blue (MB) dye, where (PL-Sp) removed MB dye effectively. Further the PL-Sp was used to produce a nanoconjugate loaded with curcumin and it was characterized using UV-Vis spectrophotometer, FT-IR, SEM-EDX, XRD, VSM and Zeta potential. It showed a sustained drug release pattern and also found to have good antibacterial and anticancer activity.
    Matched MeSH terms: Drug Delivery Systems
  8. Vyas T, Rapalli VK, Chellappan DK, Dua K, Dubey SK, Singhvi G
    Life Sci, 2021 Dec 15;287:120148.
    PMID: 34785190 DOI: 10.1016/j.lfs.2021.120148
    BACKGROUND: Biofilms are microcolonies of microbes that form communities with a variety of microbes, exhibit the same gene composition but differ in gene expression. Biofilm-associated infections have been in existence for a long, however, biofilm-associated skin disorders have not been investigated much.

    OBJECTIVES: Biofilms, which are made mostly of the matrix can be thought of as communities of microbes that are more virulent and more difficult to eradicate as compared to their planktonic counterparts. Currently, several formulations are available in the market which have the potential to treat biofilm-assisted skin disorders. However, the existing pharmacotherapies are not competent enough to cure them effectively and entirely, in several cases.

    KEY FINDINGS: Especially with the rising resistance towards antibiotics, it has become particularly challenging to ameliorate these disorders completely. The new approaches are being used to combat biofilm-associated skin disorders, some of them being photodynamic therapy, nanotherapies, and the use of novel drug delivery systems. The focus of attention, however, is nanotherapy. Micelles, solid lipid nanoparticles, quatsomes, and many others are being considered to find a better solution for the biofilm-associated skin disorders.

    SIGNIFICANCE: This review is an attempt to give a perspective on these new approaches for treating bacterial biofilms associated with skin disorders.

    Matched MeSH terms: Drug Delivery Systems/methods*; Drug Delivery Systems/trends
  9. Khan MUA, Haider S, Raza MA, Shah SA, Razak SIA, Kadir MRA, et al.
    Int J Biol Macromol, 2021 Dec 01;192:820-831.
    PMID: 34648803 DOI: 10.1016/j.ijbiomac.2021.10.033
    Carbohydrate polymers are biological macromolecules that have sparked a lot of interest in wound healing due to their outstanding antibacterial properties and sustained drug release. Arabinoxylan (ARX), Chitosan (CS), and reduced graphene oxide (rGO) sheets were combined and crosslinked using tetraethyl orthosilicate (TEOS) as a crosslinker to fabricate composite hydrogels and assess their potential in wound dressing for skin wound healing. Fourier-transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), atomic force microscopy (AFM), transmission electron microscopy (TEM), and biological assays were used to evaluate the composite hydrogels. FTIR validated the effective fabrication of the composite hydrogels. The rough morphologies of the composite hydrogels were revealed by SEM and AFM (as evident from the Ra values). ATC-4 was discovered to have the roughest surface. TEM revealed strong homogeneous anchoring of the rGO to the polymer matrix. However, with higher amount of rGO agglomeration was detected. The % swelling at various pHs (1-13) revealed that the hydrogels were pH-sensitive. The controlled release profile for the antibacterial drug (Silver sulfadiazine) evaluated at various pH values (4.5, 6.8, and 7.4) in PBS solution and 37 °C using the Franz diffusion method revealed maximal drug release at pH 7.4 and 37 °C. The antibacterial efficacy of the composite hydrogels against pathogens that cause serious skin diseases varied. The MC3T3-E1 cell adhered, proliferated, and differentiated well on the composite hydrogels. MC3T3-E1 cell also illustrated excellent viability (91%) and proper cylindrical morphologies on the composite hydrogels. Hence, the composite hydrogels based on ARX, CS, and rGO are promising biomaterials for treating and caring for skin wounds.
    Matched MeSH terms: Drug Delivery Systems
  10. Prasher P, Sharma M, R Wich P, Jha NK, Singh SK, Chellappan DK, et al.
    Future Med Chem, 2021 12;13(23):2027-2031.
    PMID: 34596425 DOI: 10.4155/fmc-2021-0218
    Matched MeSH terms: Drug Delivery Systems
  11. Shin Low S, Nong Lim C, Yew M, Siong Chai W, Low LE, Manickam S, et al.
    Ultrason Sonochem, 2021 Dec;80:105805.
    PMID: 34706321 DOI: 10.1016/j.ultsonch.2021.105805
    Recent advances in ultrasound (US) have shown its great potential in biomedical applications as diagnostic and therapeutic tools. The coupling of US-assisted drug delivery systems with nanobiomaterials possessing tailor-made functions has been shown to remove the limitations of conventional drug delivery systems. The low-frequency US has significantly enhanced the targeted drug delivery effect and efficacy, reducing limitations posed by conventional treatments such as a limited therapeutic window. The acoustic cavitation effect induced by the US-mediated microbubbles (MBs) has been reported to replace drugs in certain acute diseases such as ischemic stroke. This review briefly discusses the US principles, with particular attention to the recent advancements in drug delivery applications. Furthermore, US-assisted drug delivery coupled with nanobiomaterials to treat different diseases (cancer, neurodegenerative disease, diabetes, thrombosis, and COVID-19) are discussed in detail. Finally, this review covers the future perspectives and challenges on the applications of US-mediated nanobiomaterials.
    Matched MeSH terms: Drug Delivery Systems*
  12. Gulati N, Chellappan DK, MacLoughlin R, Dua K, Dureja H
    Life Sci, 2021 Nov 15;285:119969.
    PMID: 34547339 DOI: 10.1016/j.lfs.2021.119969
    Inflammatory lung diseases related morbidity and mortality impose a significant financial burden. Inflammation is a hallmark of many diseases of the respiratory system which is directly or indirectly linked to adverse health conditions, air pollution, rapid lifestyle changes, and regular outbreaks of microbial infections. The unique anatomical and physiological features of the lungs make them an ideal target organ in the treatment of inflammatory respiratory disease and with the help of inhaled therapy lungs can be targeted directly. The principal objective of this review is to present the comprehensive role of inhaled nano-based therapeutics such as liposomes, niosomes, nanoparticles, nanoemulsion, nanosuspension, and exosomes in the treatment and management of inflammatory respiratory diseases. Inhaled nanomedicines provide targeted diagnosis and treatment, improved drug solubility and distribution, prevent first-pass hepatic metabolism, improved patient compliance, and reduced drug side effects. They overcome several biological barriers in the human body and provide immediate, and quick-onset of action. Future research should be focused on improving the therapeutic efficiency of inhaled nanocarriers and to carry out in-depth mechanistic studies to translate current scientific knowledge for the efficient management of inflammatory lung diseases with minimal or no toxicity.
    Matched MeSH terms: Drug Delivery Systems
  13. Mohamed Sofian Z, Harun N, Mahat MM, Nor Hashim NA, Jones SA
    Eur J Pharm Biopharm, 2021 Nov;168:53-61.
    PMID: 34455038 DOI: 10.1016/j.ejpb.2021.08.003
    Transiently associating amines with therapeutic agents through the formation of ion-pairs has been established both in vitro and in vivo as an effective means to systemically direct drug delivery to the lung via the polyamine transport system (PTS). However, there remains a need to better understand the structural traits required for effective PTS uptake of drug ion-pairs. This study aimed to use a structurally related series of amine counterions to investigate how they influenced the stability of theophylline ion-pairs and their active uptake in A549 cells. Using ethylamine (mono-amine), ethylenediamine (di-amine), spermidine (tri-amine) and spermine (tetra-amine) as counterions the ion-pair affinity was shown to increase as the number of protonated amine groups in the counterion structure increased. The mono and diamines generated a single hydrogen bond and the weakest ion-pair affinities (pKFTIR: 1.32 ± 0.04 and 1.43 ± 0.02) whereas the polyamines produced two hydrogen bonds and thus the strongest ion-pair affinities (pKFTIR: 1.93 ± 0.05 and 1.96 ± 0.04). In A549 cells depleted of endogenous polyamines using α-difluoromethylornithine (DFMO), the spermine-theophylline uptake was significantly increased (p drug. As the data indicated that polyamines with at least 3 amines were required to form ion-pairs that could enhance A549 cell uptake, it suggested that at least two amines were required to physically stabilise the ion-pair and one to interact with the PTS.
    Matched MeSH terms: Drug Delivery Systems*
  14. Devkota HP, Paudel KR, Jha NK, Gupta PK, Singh SK, Chellappan DK, et al.
    Nanomedicine (Lond), 2021 11;16(27):2407-2410.
    PMID: 34670398 DOI: 10.2217/nnm-2021-0275
    Matched MeSH terms: Drug Delivery Systems
  15. Khursheed R, Singh SK, Wadhwa S, Gulati M, Kapoor B, Jain SK, et al.
    Int J Biol Macromol, 2021 Oct 31;189:744-757.
    PMID: 34464640 DOI: 10.1016/j.ijbiomac.2021.08.170
    The role of mushroom polysaccharides and probiotics as pharmaceutical excipients for development of nanocarriers has never been explored. In the present study an attempt has been made to explore Ganoderma lucidum extract powder (GLEP) containing polysaccharides and probiotics to convert liquid self nanoemulsifying drug delivery system (SNEDDS) into solid free flowing powder. Two lipophilic drugs, curcumin and quercetin were used in this study due to their dissolution rate limited oral bioavailability and poor permeability. These were loaded into liquid SNEDDS by dissolving them into isotropic mixture of Labrafill M1944CS, Capmul MCM, Tween-80 and Transcutol P. The liquid SNEDDS were solidified using probiotics and mushroom polysaccharides as carriers and Aerosil-200 as coating agent. The solidification was carried out using spray drying process. The process and formulation variables for spray drying process of liquid SNEDDS were optimized using Box Behnken Design to attain required powder properties. The release of both drugs from the optimized spray dried (SD) formulation was found to be more than 90%, whereas, it was less than 20% for unprocessed drugs. The results of DSC, PXRD and SEM, showed that the developed L-SNEDDS preconcentrate was successfully loaded onto the porous surface of probiotics, mushroom polysaccharides and Aerosil-200.
    Matched MeSH terms: Drug Delivery Systems*
  16. Gupta G, Chellappan DK, Singh SK, Gupta PK, Kesari KK, Jha NK, et al.
    Nanomedicine (Lond), 2021 10;16(25):2243-2247.
    PMID: 34547920 DOI: 10.2217/nnm-2021-0254
    Matched MeSH terms: Drug Delivery Systems*
  17. Yang CL, Chao YJ, Wang HC, Hou YC, Chen CG, Chang CC, et al.
    Nanomedicine, 2021 10;37:102450.
    PMID: 34332115 DOI: 10.1016/j.nano.2021.102450
    Epigenetic inhibitors have shown anticancer effects. Combination chemotherapy with epigenetic inhibitors has shown high effectiveness in gastric cancer clinical trials, but severe side effect and local progression are the causes of treatment failure. Therefore, we sought to develop an acidity-sensitive drug delivery system to release drugs locally to diminish unfavorable outcome of gastric cancer. In this study, we showed that, as compared with single agents, combination treatment with the demethylating agent 5'-aza-2'-deoxycytidine and HDAC inhibitors Trichostatin A or LBH589 decreased cell survival, blocked cell cycle by reducing number of S-phase cells and expression of cyclins, increased cell apoptosis by inducing expression of Bim and cleaved Caspase 3, and reexpressed tumor suppressor genes more effectively in MGCC3I cells. As a carrier, reconstituted apolipoprotein B lipoparticles (rABLs) could release drugs in acidic environments. Orally administrated embedded drugs not only showed inhibitory effects on gastric tumor growth in a syngeneic orthotopic mouse model, but also reduced the hepatic and renal toxicity. In conclusion, we have established rABL-based nanoparticles embedded epigenetic inhibitors for local treatment of gastric cancer, which have good therapeutic effects but do not cause severe side effects.
    Matched MeSH terms: Drug Delivery Systems*
  18. Ahmad S, Al-Hatamleh MAI, Mohamud R
    Cell Immunol, 2021 10;368:104412.
    PMID: 34340162 DOI: 10.1016/j.cellimm.2021.104412
    Autoimmunity is the assault of immune response towards self-antigens, resulting to inflammation and tissue injury. It is staged into three phases and caused by malfunction of immune tolerance. In our body, immune tolerance is synchronized by several immunosuppressor cells such as regulatory T cells and B cells as well as myeloid-derived suppressor cells, which are prominently dysregulated in autoimmunity. Hence, targeting these cell populations serve as a significant potential in the therapy of autoimmunity. Nanotechnology with its advantageous properties is shown to be a remarkable tool as drug delivery system in this field. This review focused on the development of therapeutics in autoimmune diseases utilizing various nanoparticles formulation based on two targeting approaches in autoimmunity, passive and active targeting. Lastly, this review outlined the approved present nanomedicines as well as in clinical evaluations and issues regarding the lack of translation of these nanomedicines into the market, despite the abundant of positive experimental observations.
    Matched MeSH terms: Drug Delivery Systems
  19. Mustafa IF, Hussein MZ, Idris AS, Hilmi NHZ, Fakurazi S
    Molecules, 2021 Sep 26;26(19).
    PMID: 34641379 DOI: 10.3390/molecules26195837
    Reports on fungicide-based agronanochemicals in combating disastrous basal stem rot disease in the oil palm industry are scant. Herein, we describe the potential of fungicide nanodelivery agents based on hexaconazole-micelle systems produced using three different surfactants; sodium dodecylbenze sulfonate (SDBS), sodium dodecyl sulfate (SDS) and Tween 80 (T80). The resulting nanodelivery systems were characterized and the results supported the encapsulation of the fungicide into the micelles of the surfactants. We have investigated in detail the size-dependent effects of the as-synthesized micelles towards the inhibition growth of Ganoderma Boninense fungi. All the nanodelivery systems indicate that their size decreased as the surfactant concentration was increased, and it directly affects the fungal inhibition. It was also found that Tween 80, a non-ionic surfactant gave the lowest effective concentration, the EC50 value of 2, on the pathogenic fungus Ganoderma boninense compared to the other anionic surfactants; SDBS and SDS. This study opens up a new generation of agronanofungicide of better efficacy for Ganoderma disease treatment.
    Matched MeSH terms: Drug Delivery Systems*
  20. Gadhave D, Tupe S, Tagalpallewar A, Gorain B, Choudhury H, Kokare C
    Int J Pharm, 2021 Sep 25;607:121050.
    PMID: 34454028 DOI: 10.1016/j.ijpharm.2021.121050
    Unfavorable side effects of available antipsychotics limit the use of conventional delivery systems, where limited exposure of the drugs to the systemic circulation could reduce the associated risks. The potential of intranasal delivery is gaining interest to treat brain disorders by delivering the drugs directly to the brain circumventing the tight junctions of the blood-brain barrier with limited systemic exposure of the entrapped therapeutic. Therefore, the present research was aimed to fabricate, optimize and investigate the therapeutic efficacy of amisulpride (AMS)-loaded intranasal in situ nanoemulgel (AMS-NG) in the treatment of schizophrenia. In this context, AMS nanoemulsion (AMS-NE) was prepared by employing aqueous-titration method and optimized using Box-Behnken statistical design. The optimized nanoemulsion was subjected to evaluation of globule size, transmittance, zeta potential, and mucoadhesive strength, which were found to be 92.15 nm, 99.57%, -18.22 mV, and 8.90 g, respectively. The AMS-NE was converted to AMS-NG using poloxamer 407 and gellan gum. Following pharmacokinetic evaluation in Wistar rats, the brain Cmax for intranasal AMS-NG was found to be 1.48-folds and 3.39-folds higher when compared to intranasal AMS-NE and intravenous AMS-NE, respectively. Moreover, behavioral investigations of developed formulations were devoid of any extrapyramidal side effects in the experimental model. Finally, outcomes of the in vivo hematological study confirmed that intranasal administration of formulation for 28 days did not alter leukocytes and agranulocytes count. In conclusion, the promising results of the developed and optimized intranasal AMS-NG could provide a novel platform for the effective and safe delivery of AMS in schizophrenic patients.
    Matched MeSH terms: Drug Delivery Systems
Filters
Contact Us

Please provide feedback to Administrator (afdal@afpm.org.my)

External Links