Displaying publications 61 - 80 of 233 in total

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  1. Fulltext Microwave-assisted Preparation of Cross-linked Gelatin-Paracetamol Matrices: Optimization Using the D-optimal Design
    Kuang TK, Kang YB, Segarra I, Kanwal U, Ahsan M, Bukhari NI
    Turk J Pharm Sci, 2021 04 20;18(2):167-175.
    PMID: 33902255 DOI: 10.4274/tjps.galenos.2020.48902
    Objectives: This study was conducted to assess the effect of microwave heating on the preparation of paracetamol cross-linked gelatin matrices by using the design of experiment (DoE) approach and explore the influence of the duration of microwave irradiation, the concentrations of crosslinker, and the amount of sodium bicarbonate (salt) on paracetamol release. These parameters were also compared with those of the matrices prepared via conventional heating.

    Materials and Methods: Twenty gel matrices were prepared with different durations of microwave irradiation, amounts of maize, and concentrations of sodium bicarbonate as suggested by Design Expert (DX®). The percentage drug release, the coefficient of variance (CV) in release, and the mean dissolution time (MDT) were the properties explored in the designed experimentation.

    Results: Target responses were dependent on microwave irradiation time, cross-linker amount, and salt concentration. Classical and microwave heating did not demonstrate statistically significant difference in modifying the percentage of drug released from the matrices. However, the CVs of microwave-assisted formulations were lower than those of the gel matrices prepared via classical heating. Thus, microwave heating produced lesser variations in drug release. The optimized gel matrices demonstrated that the observed percentage of drug release, CV, and MDT were within the prediction interval generated by DX®. The release mechanism of the matrix formulations followed the Peppas-Korsmeyer anomalous transport model.

    Conclusion: The DoE-supported microwave-assisted approach could be applied to optimize the critical factors of drug release with less variation.

    Matched MeSH terms: Drug Liberation
  2. Topological characterization of a bacterial cellulose-acrylic acid polymeric matrix
    Halib N, Mohd Amin MC, Ahmad I, Abrami M, Fiorentino S, Farra R, et al.
    Eur J Pharm Sci, 2014 Oct 1;62:326-33.
    PMID: 24932712 DOI: 10.1016/j.ejps.2014.06.004
    This paper focuses on the micro- and nano-topological organization of a hydrogel, constituted by a mixture of bacterial cellulose and acrylic acid, and intended for biomedical applications. The presence of acrylic acid promotes the formation of two interpenetrated continuous phases: the primary "pores phase" (PP) containing only water and the secondary "polymeric network phase" (PNP) constituted by the polymeric network swollen by the water. Low field Nuclear Magnetic Resonance (LF NMR), rheology, Scanning Electron Microscopy (SEM) and release tests were used to determine the characteristics of the two phases. In particular, we found that this system is a strong hydrogel constituted by 81% (v/v) of PP phase the remaining part being occupied by the PNP phase. Pores diameters span in the range 10-100 μm, the majority of them (85%) falling in the range 30-90 μm. The high PP phase tortuosity indicates that big pores are not directly connected to each other, but their connection is realized by a series of interconnected small pores that rend the drug path tortuous. The PNP is characterized by a polymer volume fraction around 0.73 while mesh size is around 3 nm. The theoretical interpretation of the experimental data coming from the techniques panel adopted, yielded to the micro- and nano-organization of our hydrogel.
    Matched MeSH terms: Drug Liberation
  3. Fulltext Follicle Stimulating Hormone (FSH) Dosage Based on Body Weight Enhances Ovulatory Responses and Subsequent Embryo Production in Goats
    Rahman MR, Rahman MM, Wan Khadijah WE, Abdullah RB
    Asian-Australas J Anim Sci, 2014 Sep;27(9):1270-4.
    PMID: 25178370 DOI: 10.5713/ajas.2013.13786
    An experiment was conducted to evaluate the efficacy of porcine follicle stimulating hormone (pFSH) dosage based on body weight (BW) on ovarian responses of crossbred does. Thirty donor does were divided into 3 groups getting pFSH dosages of 3, 5, and 8 mg pFSH per kg BW, respectively, and were named as pFSH-3, pFSH-5 and pFSH-8, respectively. Estrus was synchronized by inserting a controlled internal drug release (CIDR) device and a single injection of prostaglandin F2α (PGF2α). The pFSH treatments were administered twice a day through 6 decreasing dosages (25, 25, 15, 15, 10, and 10% of total pFSH amount; decreasing daily). Ovarian responses were evaluated on Day 7 after CIDR removal. After CIDR removal, estrus was observed 3 times in a day and pFSH treatments were initiated at 2 days before the CIDR removal. All does in pFSH-5 and pFSH-8 showed estrus signs while half of the does in pFSH-3 showed estrus signs. No differences (p>0.05) were observed on the corpus luteum and total ovarian stimulation among the treatment groups, while total and transferable embryos were higher (p<0.05) in pFSH-5 (7.00 and 6.71) than pFSH-3 (3.00 and 2.80) and pFSH-8 (2.00 and 1.50), respectively. In conclusion, 5 mg pFSH per kg BW dosage gave a higher number of embryos than 3 and 8 mg pFSH per kg BW dosages. The results indicated that the dosage of pFSH based on BW is an important consideration for superovulation in goats.
    Matched MeSH terms: Drug Liberation
  4. Fulltext Novel swellable polymer of orchidaceae family for gastroretentive drug delivery of famotidine
    Razavi M, Nyamathulla S, Karimian H, Noordin MI
    Drug Des Devel Ther, 2014;8:1315-29.
    PMID: 25246773 DOI: 10.2147/DDDT.S68517
    This study aimed to develop hydrophilic, gastroretentive matrix tablets of famotidine with good floating and swelling properties. A novel gastroretentive drug delivery formulation was designed using salep, also known as salepi, a flour obtained from grinding dried palmate tubers of Orchis morio var mascula (Orchidaceae family). The main polysaccharide content of salep is glucomannan, highly soluble in cold and hot water, which forms a viscous solution. Salep was characterized for physicochemical properties, thermal stability, chemical interaction, and surface morphology using X-ray diffraction analysis, differential scanning calorimetry, Fourier transform infrared spectroscopy, and scanning electron microscopy. Ten different formulations (S1-S10) were prepared using famotidine to salep ratios from 1:0.5 to 1:5. Results demonstrated that all formulations were able to sustain the drug release for more than 24 hours. The S5 formulation, with a famotidine to salep ratio of 1:2.5, had the shortest floating lag time of 35 seconds and 100% drug release within 24 hours. The dissolution data were fitted into popular mathematical models to assess the mechanism of drug release. S5 showed Zero order release (R=0.9746) with Higuchi diffusion (R=0.9428). We conclude that salep, a novel polymer, can be used in controlled release formulations to sustain release for 24 hours, due to inherent swelling and gelling properties.
    Matched MeSH terms: Drug Liberation
  5. Development of biofilm-targeted antimicrobial wound dressing for the treatment of chronic wound infections
    Ng SF, Leow HL
    Drug Dev Ind Pharm, 2015;41(11):1902-9.
    PMID: 25758412 DOI: 10.3109/03639045.2015.1019888
    It has been established that microbial biofilms are largely responsible for the recalcitrance of many wound infections to conventional antibiotics. It was proposed that the efficacy of antibiotics could be optimized via the inhibition of bacterial biofilm growth in wounds. The combination of antibiofilm agent and antibiotics into a wound dressing may be a plausible strategy in wound infection management. Xylitol is an antibiofilm agent that has been shown to inhibit the biofilm formation. The purpose of this study was to develop an alginate film containing xylitol and gentamicin for the treatment of wound infection. Three films, i.e. blank alginate film (SA), alginate film with xylitol (F5) and alginate film with xylitol and gentamicin (AG), were prepared. The films were studied for their physical properties, swelling ratio, moisture absorption, moisture vapor transmission rate (MVTR), mechanical and rheology properties, drug content uniformity as well as in vitro drug release properties. Antimicrobial and antibiofilm in vitro studies on Staphylococcus aureus and Pseudomonas aeruginosa were also performed. The results showed that AG demonstrates superior mechanical properties, rheological properties and a higher MVTR compared with SA and F5. The drug flux of AG was higher than that of commercial gentamicin cream. Furthermore, antimicrobial studies showed that AG is effective against both S. aureus and P. aeruginosa, and the antibiofilm assays demonstrated that the combination was effective against biofilm bacteria. In summary, alginate films containing xylitol and gentamicin may potentially be used as new dressings for the treatment of wound infection.
    Matched MeSH terms: Drug Liberation
  6. Fulltext Formulation development and dissolution rate enhancement of efavirenz by solid dispersion systems
    Koh PT, Chuah JN, Talekar M, Gorajana A, Garg S
    Indian J Pharm Sci, 2013 May;75(3):291-301.
    PMID: 24082345 DOI: 10.4103/0250-474X.117434
    The aim of this study was to enhance the dissolution rate of efavirenz using solid dispersion systems (binary and ternary). A comparison between solvent and fusion method was also investigated. Solid dispersions of efavirenz were prepared using polyethylene glycol 8000, polyvinylpyrrolidone K30 alone and combination of both. Tween 80 was incorporated to obtain a ternary solid dispersion system. Dissolution tests were conducted and evaluated on the basis of cumulative percentage drug release and dissolution efficiency. Physicochemical characterizations of the solid dispersions were carried out using differential scanning calorimetric, powder X-ray diffraction, Fourier transform infrared spectroscopy, and scanning electron microscopy. Dissolution was remarkably improved in both systems compared to pure efavirenz (P<0.05). An optimum ratio was identified at a drug:polymer of 1:10. Incorporation of Tween 80 to 1:10 formulations formed using solvent method showed further improvement in the dissolution rate. Physicochemical characterization results suggested that efavirenz existed in the amorphous form in all the solid dispersion systems providing evidence of improvement in dissolution. No statistically significant difference (P>0.05) in dissolution was observed between the two methods. Binary and ternary solid dispersion systems both have showed a significant improvement in the dissolution rate of efavirenz. Formulations with only polyvinylpyrrolidone K30 showed best dissolution profile and 1:10 was identified as an optimum drug-polymer weight ratio.
    Matched MeSH terms: Drug Liberation
  7. Fulltext Formulation development and optimization of sustained release matrix tablet of Itopride HCl by response surface methodology and its evaluation of release kinetics
    Bose A, Wong TW, Singh N
    Saudi Pharm J, 2013 Apr;21(2):201-13.
    PMID: 23960836 DOI: 10.1016/j.jsps.2012.03.006
    The objective of this present investigation was to develop and formulate sustained release (SR) matrix tablets of Itopride HCl, by using different polymer combinations and fillers, to optimize by Central Composite Design response surface methodology for different drug release variables and to evaluate drug release pattern of the optimized product. Sustained release matrix tablets of various combinations were prepared with cellulose-based polymers: hydroxy propyl methyl cellulose (HPMC) and polyvinyl pyrolidine (pvp) and lactose as fillers. Study of pre-compression and post-compression parameters facilitated the screening of a formulation with best characteristics that underwent here optimization study by response surface methodology (Central Composite Design). The optimized tablet was further subjected to scanning electron microscopy to reveal its release pattern. The in vitro study revealed that combining of HPMC K100M (24.65 MG) with pvp(20 mg)and use of LACTOSE as filler sustained the action more than 12 h. The developed sustained release matrix tablet of improved efficacy can perform therapeutically better than a conventional tablet.
    Matched MeSH terms: Drug Liberation
  8. Fulltext Formulation and evaluation of voriconazole ophthalmic solid lipid nanoparticles in situ gel
    Pandurangan DK, Bodagala P, Palanirajan VK, Govindaraj S
    Int J Pharm Investig, 2016 Jan-Mar;6(1):56-62.
    PMID: 27014620 DOI: 10.4103/2230-973X.176488
    In the present investigation, solid lipid nanoparticles (SLNs)-loaded in situ gel with voriconazole drug was formulated. Further, the formulation was characterized for pH, gelling capacity, entrapment efficiency, in vitro drug release, drug content, and viscosity. Voriconazole is an antifungal drug used to treat various infections caused by yeast or other types of fungi. Film hydration technique was used to prepared SLNs from lecithin and cholesterol. Based on the entrapment efficiency 67.2-97.3% and drug release, the optimized formulation NF1 of SLNs was incorporated into in situ gels. The in situ gels were prepared using viscosity-enhancing polymers such as Carbopol and (hydroxypropyl)methyl cellulose (HPMC). Formulated SLN in situ gel formulations were characterized, which showed pH 4.9-7.1, drug content 65.69-96.3%, and viscosity (100 rpm) 120-620 cps. From the characterizations given above, F6 was optimized and evaluated for microbial assay and ocular irritation studies. Microbial assay was conducted by the cup-plate method using Candida albicans as the test organism. An ocular irritation study was conducted on albino rabbits. The results revealed that there was no ocular damage to the cornea, conjunctiva, or iris. Stability studies were carried out on the F6 formulation for 3 months, which showed that the formulation had good stability. These results indicate that the studied SLNs-loaded in situ gel is a promising vehicle for ocular delivery.
    Matched MeSH terms: Drug Liberation
  9. Development and in vitro assessment of alginate bilayer films containing the olive compound hydroxytyrosol as an alternative for topical chemotherapy
    Ng SF, Tan SL
    Int J Pharm, 2015 Nov 30;495(2):798-806.
    PMID: 26434999 DOI: 10.1016/j.ijpharm.2015.09.057
    Topical chemotherapy is the application of cancer drugs directly onto the skin, which has become a standard treatment for basal cell carcinoma. Due to the promising results in the treatment of skin cancer, topical chemotherapy has recently been applied to breast cancer patients because some breast cancer tissues are only superficial. Hydroxytyrosol, a phenolic compound from olives that is present in high amounts in Hidrox(®) olive extract, has been shown to have a protective effect on normal cells and selective antitumor activities on cancerous cells. The aims of the present study were to develop an alginate bilayer film containing Hidrox(®) and to investigate its potential use as a topical chemotherapeutic agent. Alginate films were characterized for swelling and for physical, thermal, rheological, and mechanical properties. Drug content uniformity and in vitro drug release tests were also investigated. The alginate bilayer films containing Hidrox(®), HB2, showed controlled release of hydroxytyrosol at a flux of 0.094±0.009 mg/cm(2)/h. The results of the cytotoxic assay showed that the HB2 films were dose-dependent and could significantly reduce the growth of breast cancer cells (MCF-7) at 150 μg/mL for a cell viability of 29.34±4.64%. In conclusion, an alginate bilayer film containing Hidrox(®) can be a potential alternative for topical chemotherapeutic agent for skin and breast cancer treatment.
    Matched MeSH terms: Drug Liberation
  10. Chitosan modified 5-fluorouracil nanostructured lipid carriers for treatment of diabetic retinopathy in rats: A new dimension to an anticancer drug
    Sharma DS, Wadhwa S, Gulati M, Kumar B, Chitranshi N, Gupta VK, et al.
    Int J Biol Macromol, 2023 Jan 01;224:810-830.
    PMID: 36302483 DOI: 10.1016/j.ijbiomac.2022.10.168
    Diabetic retinopathy (DR) is one of the chronic complications of diabetes. It includes retinal blood vessels' damage. If untreated, it leads to loss of vision. The existing treatment strategies for DR are expensive, invasive, and need expertise during administration. Hence, there is a need to develop a non-invasive topical formulation that can penetrate deep to the posterior segment of retina and treat the damaged retinal vessels. In addition, it should also provide sustained release. In recent years, novel drug delivery systems (NDDS) have been explored for treating DR and found successful. In this study, chitosan (CS) modified 5-Fluorouracil Nanostructured Lipid Carriers (CS-5-FU-NLCs) were prepared by modified melt emulsification-ultrasonication method and optimized by Box-Behnken Design. The size, polydispersity index, zeta potential and entrapment efficiency of CS-5-FU-NLCs were 163.2 ± 2.3 nm, 0.28 ± 1.52, 21.4 ± 0.5 mV and 85.0 ± 0.2 %, respectively. The in vitro drug release and ex vivo permeation study confirmed higher and sustained drug release in CS-5-FU-NLCs as compared to 5-FU solution. HET-CAM Model ensured the non-irritant nature of CS-5-FU-NLCs. In vivo ocular studies of CS-5-FU-NLCs confirmed antiangiogenic effect of 5-FU by CAM model and diabetic retinopathy induced rat model, indicating successful delivery of 5-FU to the retina.
    Matched MeSH terms: Drug Liberation
  11. Fulltext Stimuli-responsive liposomal nanoformulations in cancer therapy: Pre-clinical & clinical approaches
    Ashrafizadeh M, Delfi M, Zarrabi A, Bigham A, Sharifi E, Rabiee N, et al.
    J Control Release, 2022 Nov;351:50-80.
    PMID: 35934254 DOI: 10.1016/j.jconrel.2022.08.001
    The site-specific delivery of antitumor agents is of importance for providing effective cancer suppression. Poor bioavailability of anticancer compounds and the presence of biological barriers prevent their accumulation in tumor sites. These obstacles can be overcome using liposomal nanostructures. The challenges in cancer chemotherapy and stimuli-responsive nanocarriers are first described in the current review. Then, stimuli-responsive liposomes including pH-, redox-, enzyme-, light-, thermo- and magneto-sensitive nanoparticles are discussed and their potential for delivery of anticancer drugs is emphasized. The pH- or redox-sensitive liposomes are based on internal stimulus and release drug in response to a mildly acidic pH and GSH, respectively. The pH-sensitive liposomes can mediate endosomal escape via proton sponge. The multifunctional liposomes responsive to both redox and pH have more capacity in drug release at tumor site compared to pH- or redox-sensitive alone. The magnetic field and NIR irradiation can be exploited for external stimulation of liposomes. The light-responsive liposomes release drugs when they are exposed to irradiation; thermosensitive-liposomes release drugs at a temperature of >40 °C when there is hyperthermia; magneto-responsive liposomes release drugs in presence of magnetic field. These smart nanoliposomes also mediate co-delivery of drugs and genes in synergistic cancer therapy. Due to lack of long-term toxicity of liposomes, they can be utilized in near future for treatment of cancer patients.
    Matched MeSH terms: Drug Liberation
  12. Chitosan coated magnetic cellulose nanowhisker as a drug delivery system for potential colorectal cancer treatment
    Yusefi M, Shameli K, Lee-Kiun MS, Teow SY, Moeini H, Ali RR, et al.
    Int J Biol Macromol, 2023 Apr 01;233:123388.
    PMID: 36706873 DOI: 10.1016/j.ijbiomac.2023.123388
    Polysaccharide-based magnetic nanocomposites can eminently illuminate several attractive features as anticancer drug carriers. In this study, rice straw-based cellulose nanowhisker (CNW) was used as solid support for Fe3O4 nanofillers to synthesize magnetic CNW. Then, cross-linked chitosan-coated magnetic CNW for 5-fluorouracil carrier abbreviated as CH/MCNW/5FU. Fourier-transform infrared, X-Ray diffraction, and X-ray photoelectron spectroscopy analysis indicated successful fabrication and multifunctional properties of the CH/MCNW/5FU nanocomposites. In addition, CH/MCNW/5FU nanocomposites showed hydrodynamic diameter and zeta potential value of 181.31 ± 3.46 nm and +23 ± 1.8 mV, respectively. Based on images of transmission electron microscopy, magnetic CNW as reinforcement was coated with chitosan to obtain almost spherical CH/MCNW/5FU nanocomposites with an average diameter of 37.16 ± 3.08. The nanocomposites indicated desired saturation magnetization and thermal stability, high drug encapsulation efficiency, and pH-dependent swelling and drug release performance. CH/MCNW/5FU nanocomposites showed potent killing effects against colorectal cancer cells in both 2D monolayer and 3D spheroid models. These findings suggest CH/MCNW as a potential carrier for anticancer drugs with high tumour-penetrating capacity.
    Matched MeSH terms: Drug Liberation
  13. Fulltext Investigating the in-vitro bioactivity, biodegradability and drug release behavior of the newly developed PES/HA/WS biocompatible nanocomposites as bone graft substitute
    Salimi E, Asim MH, Abidin MNZ
    Sci Rep, 2024 May 11;14(1):10798.
    PMID: 38734777 DOI: 10.1038/s41598-024-61586-2
    The nucleation of carbonate-containing apatite on the biomaterials surface is regarded as a significant stage in bone healing process. In this regard, composites contained hydroxyapatite (Ca10(PO4)6(OH)2, HA), wollastonite (CaSiO3, WS) and polyethersulfone (PES) were synthesized via a simple solvent casting technique. The in-vitro bioactivity of the prepared composite films with different weight ratios of HA and WS was studied by placing the samples in the simulated body fluid (SBF) for 21 days. The results indicated that the the surface of composites containing 2 wt% HA and 4 wt% WS was completely covered by a thick bone-like apatite layer, which was characterized by Grazing incidence X-ray diffraction, attenuated total reflectance-Fourier transform infrared spectrometer, field emission electron microscopy and energy dispersive X-ray analyzer (EDX). The degradation study of the samples showed that the concentration of inorganic particles could not influence the degradability of the polymeric matrix, where all samples expressed similar dexamethasone (DEX) release behavior. Moreover, the in-vitro cytotoxicity results indicated the significant cyto-compatibility of all specimens. Therefore, these findings revealed that the prepared composite films composed of PES, HA, WS and DEX could be regarded as promising bioactive candidates with low degradation rate for bone tissue engineering applications.
    Matched MeSH terms: Drug Liberation
  14. Using Quality by Design Tools to Study Gel Formulation from Brassica juncea Leaves and Conducting its In vitro, In vivo, Molecular Docking, and ADMET Analyses
    Kanakal MM, Abbas SA, Khan A, Sultana S, Fatima H, Tabasssum R, et al.
    Antiinflamm Antiallergy Agents Med Chem, 2024;23(3):187-204.
    PMID: 39082166 DOI: 10.2174/0118715230309053240718122527
    INTRODUCTION: This research aims to create a gel formulation of Brassica juncea leaf extract and assess its anti-inflammatory properties using an in silico study. The anti-inflammatory activity has been compared with Diclofenac molecules in PDB id: 4Z69. Further, the Absorption, Distribution, Metabolism, Excretion, and Toxicity analysis has been performed to ensure the therapeutic potential and safety of the drug development process. The Quality by Design tool has been applied to optimize formulation development.

    METHODS: The extracted gel is characterized by performing Fourier transformer infrared, zeta potential, particle size, Scanning Electron Microscope, and entrapment efficiency. Further, the formulation is evaluated by examining its viscosity, spreadability, and pH measurement. An In vitro study of all nine extract suspensions was conducted to determine the drug contents at 276 nm.

    RESULTS: The optimized suspension has shown the maximum percentage of drug release (82%) in 10 hours of study. Animal study for anti-inflammatory activity was performed, and results of all five groups of animals compared the % inhibition of paw edema at three hours; gel (56.70%), standard (47.86%), and (39.72%) were found.

    CONCLUSION: The research could conclude that the anti-inflammatory activity of gel formulation is high compared to extract, and a molecular docking study validates the anti-inflammatory therapeutic effects. ADMET analysis ensures the therapeutic effects and their safety.

    Matched MeSH terms: Drug Liberation
  15. Fulltext Development and characterization of a self-nano emulsifying drug delivery system (SNEDDS) for Ornidazole to improve solubility and oral bioavailability of BCS class II drugs
    Mohite P, Sule S, Pawar A, Alharbi HM, Maitra S, Subramaniyan V, et al.
    Sci Rep, 2024 Nov 12;14(1):27724.
    PMID: 39532892 DOI: 10.1038/s41598-024-73760-7
    This study aimed to investigate the in vitro performance of self-nanoemulsifying drug delivery systems (SNEDDSs) of Ornidazole (ORD), a poorly water-soluble drug. Self-nanoemulsifying drug delivery systems of ORD were prepared using various oils, non-ionic surfactants, and/or water-soluble co-solvents and assessed visually/by droplet size measurement. Equilibrium solubility of ORD in the anhydrous and diluted SNEDDS was conducted to achieve the maximum drug loading. The in vitro dissolution of SNEDDS was studied to compare the solubility of the representative formulations with API. The results from the characterization and solubility studies showed that SNEDDS formulations were stable with lower droplet sizes and showed higher ORD solubility. From the dissolution studies, it was found that the developed A7-SNEDDS formulation provided a significantly higher rate of ORD release (98.94 ± 0.68 in 1.0 h) compared to API. ORD-loaded SNEDDS formulations could be a potential oral pharmaceutical product with high drug-loading capacity, improved drug dissolution, and enhanced oral bioavailability.
    Matched MeSH terms: Drug Liberation
  16. Antioxidant and anticancer activities of hesperetin and its novel formulations in KB cells
    Chauhan A, Salwa, Shedgaonkar GG, Kumar L, Karmakar A, Khajuria S, et al.
    Naunyn Schmiedebergs Arch Pharmacol, 2025 May;398(5):5213-5236.
    PMID: 39531045 DOI: 10.1007/s00210-024-03581-y
    This study aimed to formulate the hesperetin nanostructured lipid carriers (NLCs) containing oro-mucosal gel for its activity assessment on the KB cell line. NLCs were prepared with glyceryl monostearate, oleic acid, and lecithin using a modified constant-temperature emulsification technique. The particle size analysis, in vitro drug release studies, etc., of prepared NLCs were evaluated. The formulated gels were analyzed with respect to spreadability, extrudability, swelling index, texture analysis, etc. The particle size, polydispersity index, zeta potential, and drug entrapment of nanocarriers were recorded to be 221.733 ± 61.536 nm, 0.381 ± 0.091, - 51.433 ± 4.143 mV, and 89.29%, respectively. The optimized NLCs in 24 h released 87.14 ± 6.62% of the drug. The round shape of NLCs was noticed with scanning electron microscopy. The pH, spreadability, extrudability, swelling index, content uniformity, and drug release studies of hesperetin NLCs-containing gel (HNG) were found to be 6.81 ± 0.04, 2.49 ± 0.04 cm.mg/s, 539.04 ± 32.88 g/cm2, 4.27 ± 0.47, 107.98 ± 1.93%, and 90.17 ± 6.67% (in 48 h), respectively. The developed formulations showed promising in vitro anticancer and antioxidant activities. HNP results authorize that the formulation may be beneficial for the treatment of oral cancer.
    Matched MeSH terms: Drug Liberation
  17. Quality by design approach for optimization, in-vitro and in-vivo evaluation of compression-spheronized itopride hydrochloride loaded gastroretentive pellets for the treatment of gastroesophageal reflux disease
    Dass R, Rani P, Kumar D, Choudhary N, Lohan S, Mahmood S, et al.
    Naunyn Schmiedebergs Arch Pharmacol, 2026 Feb;399(3):4305-4320.
    PMID: 41108360 DOI: 10.1007/s00210-025-04728-1
    Gastroesophageal reflux disease (GERD) is the most common disorder with a significantly high global prevalence. Prokinetic drugs are commonly recommended for the treatment of gastric reflux, in addition to antacids and antisecretory agents. Itopride hydrochloride, a prokinetic agent, acts as a D2 receptor antagonist and an acetylcholinesterase inhibitor, improving GERD symptoms. The objective of this study was to develop a floating-type gastroretentive drug delivery system, which was further evaluated by in vitro and in vivo studies. Itopride hydrochloride-loaded gastroretentive pellets were prepared using pelletization followed by spheronization. The preparation of itopride-loaded gastroretentive pellets was optimized using a central composite experimental design (32), varying the concentrations of ethylcellulose and Eudragit S100 as independent variables, while floating time and percentage of drug release were considered dependent variables.The optimized batch was characterized by X-ray diffraction (XRD), differential scanning calorimetry (DSC), and Fourier-transform infrared spectroscopy (FTIR). It was then evaluated for mucoadhesion, in vivo gastric retention, and bioavailability in rabbits. The in vitro drug release from the optimized pellet formulation exhibited approximately 97.84% release over 10 h and maintained buoyancy for up to 9 h. In vivo gastric residence time was observed to be 6 h, with a bioavailability of 52.87 ± 0.15 µg/mL/h. Based on in vitro and in vivo findings, the developed gastroretentive mucoadhesive pellet formulation presents a promising drug delivery system for the treatment of GERD, potentially enhancing drug efficacy through prolonged gastric retention.
    Matched MeSH terms: Drug Liberation
  18. Formulation and development of thymoquinone-loaded ufasome hydrogel for effective treatment of onychomycosis
    Ali MS, Rehman U, Gupta G, Alsayari A, Wahab S, Goh KW, et al.
    Naunyn Schmiedebergs Arch Pharmacol, 2026 Jan;399(1):1515-1535.
    PMID: 40813484 DOI: 10.1007/s00210-025-04505-0
    Chronic fungal nail infections like onychomycosis are challenging to treat due to drug resistance, long treatment durations, and poor nail penetration of conventional antifungals. Here, we report the formulation and evaluation of a thymoquinone-loaded ufasome hydrogel (TQ-UFs-Gel) designed for enhanced transungual delivery. TQ-UFs were prepared by thin-film hydration of sodium oleate and cholesterol, optimized via a central composite design to yield vesicles ~ 191.50 ± 0.23 nm in size with 80.05 ± 0.34% entrapment efficiency and PDI 0.18 ± 0.32. The hydrogel was formed by incorporating TQ-UFs into 1% Carbopol 940. Physicochemical characterization included pH, spreadability, viscosity, texture profile analysis, in vitro release (Franz diffusion), ex vivo bovine hoof permeation, nail clipping drug loading, and HET-CAM irritation testing. The optimized TQ-UFs-Gel exhibited shear-thinning behavior (viscosity 987 → 387 cP), pH 5.9 ± 0.23, spreadability 8.7 ± 0.12 cm, and firmness 191.7 g. In vitro release showed a biphasic profile (39.90% in 2 h; 90.10% in 24 h), fitting the Korsmeyer-Peppas model (R2 = 0.9537). Ex vivo studies demonstrated 95.20 ± 0.8% cumulative permeation and flux 3.29 µg/cm2/h, versus 70.30 ± 0.2% and 2.97 µg/cm2/h for control gel. Nail clipping analysis confirmed increased TQ loading (1.43 µg/mg vs. 0.68 µg/mg for free TQ). Antifungal assays against Trichophyton mentagrophytes showed a significant CFU reduction for TQ-UFs compared to free drug, and HET-CAM tests indicated minimal irritation (IrS 0.41 ± 1.20). TQ-UFs-Gel demonstrated sustained release, enhanced nail permeation, and antifungal activity with low irritation potential, supporting its potential as a transungual delivery system for onychomycosis treatment.
    Matched MeSH terms: Drug Liberation
  19. Green Nanotechnology for Synthesis and characterization of poly(3-hydroxybutyrate-co-3-hydroxyhexanoate) nanoparticles for sustained bortezomib release using supercritical CO2 assisted particle formation combined with electrodeposition
    Demirdöğen RE, Emen FM, Ocakoglu K, Murugan P, Sudesh K, Avşar G
    Int J Biol Macromol, 2018 Feb;107(Pt A):436-445.
    PMID: 28888547 DOI: 10.1016/j.ijbiomac.2017.09.011
    Carbon dioxide assisted particle formation combined with electrospraying using supercritical CO2 (scCO2) as an aid (Carbon Dioxide Assisted Nebulization-Electrodeposition, CAN-ED) was used to produce Bortezomib loaded poly(3-hydroxybutyrate-co-3-hydroxyhexanoate) P(3HB-co-3HHx) nanoparticles for sustained release. The morphology and structure of the prepared nanoparticles were investigated by SEM, TEM and FT-IR spectroscopy. Average diameter of particles obtained was 155nm and the average core sizes of P(3HB-co-3HHx) nanoparticles were between 6 and 13nm. The drug loading capacity, drug release and stability of Bortezomib loaded P(3HB-co-3HHx) nanoparticles were analyzed. The maximum loading capacity was achieved at pH=6.0 in phosphate buffer (K2HPO4/KH2PO4). It was found that temperature did not affect the stability of Bortezomib loaded nanoparticles and it was good both at 37°C and 4°C. This study pointed out that CAN-ED is a green method to produce P(3HB-co-3HHx) nanoparticles for pH responsive targeting of Bortezomib especially to parts of the body where size exclusion is not crucial.
    Matched MeSH terms: Drug Liberation*
  20. Rheological behavior of biodegradable N-succinyl chitosan-g-poly (acrylic acid) hydrogels and their applications as drug carrier and in vitro theophylline release
    Bashir S, Teo YY, Ramesh S, Ramesh K, Mushtaq MW
    Int J Biol Macromol, 2018 Oct 01;117:454-466.
    PMID: 29807081 DOI: 10.1016/j.ijbiomac.2018.05.182
    Novel pH sensitive N-succinyl chitosan-g-poly (acrylic acid) hydrogels were synthesized through free radical mechanism. Rheometer was used to observe the mechanical strength of the hydrogels. In vitro degradation was conducted in SIF (pH 7.4). The effect of concentration of monomers, initiator, and crosslinking agent and pH and ionic strength of NaCl, CaCl2, and AlCl3 on swelling of the hydrogels was observed. The results showed that equilibrium swelling ratio was highly influenced by concentration of monomers, initiator, and crosslinking agent concentration, and pH and salt solutions of NaCl, CaCl2, and AlCl3. The swelling kinetics revealed that swelling followed non-Fickian anomalous transport. Furthermore, theophylline loading (DL %) and encapsulation efficiency (EE %) of the hydrogels was in the range of 15.5 ± 0.15-22.8 ± 0.06% and 62 ± 0.15-91 ± 0.26%, respectively. The release of theophylline in physiological mediums was strongly influenced by the pH. The theophylline release was in the range of 51 ± 0.20-92 ± 0.12% in SIF and 7.4 ± 0.02-14.9 ± 0.03% in SGF (pH 1.2), respectively. The release data fitted well to Korsmeyer-Peppas model. The chemical activity of the theophylline suggested that drug maintained its chemical activity after release in vitro. The results suggest that synthesized hydrogels are excellent drug carriers.
    Matched MeSH terms: Drug Liberation*
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