Development of Tizanidine Drug-in-Adhesive Patch: Molecular Mechanism of Permeation Enhancer on Regulating Miscibility and Drug Release by Affecting the Status of Ion-Pair in Polymer Matrix

2020 ◽  
Vol 109 (8) ◽  
pp. 2501-2511
Author(s):  
Ting Zhong ◽  
Jiuheng Ruan ◽  
Chao Liu ◽  
Peng Quan ◽  
Liang Fang
Keyword(s):  
Drug Release ◽  
Molecular Mechanism ◽  
Polymer Matrix ◽  
Ion Pair ◽  
Permeation Enhancer ◽  
Adhesive Patch ◽  
The Status

scholarly journals The Correlation between Physical Crosslinking and Water-Soluble Drug Release from Chitosan-Based Microparticles

Pharmaceutics ◽  
2020 ◽  
Vol 12 (5) ◽  
pp. 455
Author(s):  
Emilia Szymańska ◽  
Katarzyna Woś-Latosi ◽  
Julia Jacyna ◽  
Magdalena Dąbrowska ◽  
Joanna Potaś ◽  
...  
Keyword(s):  
Drug Release ◽  
Polymer Matrix ◽  
Drug Loading ◽  
Water Soluble ◽  
Dissolution Behavior ◽  
Complex Nature ◽  
Prolonged Release ◽  
Scanning Calorimetry ◽  
Burst Effect ◽  
The Impact

Microparticles containing water-soluble zidovudine were prepared by spray-drying using chitosan glutamate and beta-glycerophosphate as an ion crosslinker (CF). The Box–Behnken design was applied to optimize the microparticles in terms of their drug loading and release behavior. Physicochemical studies were undertaken to support the results from dissolution tests and to evaluate the impact of the crosslinking ratio on the microparticles’ characteristics. The zidovudine dissolution behavior had a complex nature which comprised two phases: an initial burst effect followed with a prolonged release stage. The initial drug release, which can be modulated by the crosslinking degree, was primarily governed by the dissolution of the drug crystals located on the microparticles’ surfaces. In turn, the further dissolution stage was related to the drug diffusion from the swollen polymer matrix and was found to correlate with the drug loading. Differential Scanning Calorimetry (DSC) studies revealed the partial incorporation of a non-crystallized drug within the polymer matrix, which correlated with the amount of CF. Although CF influenced the swelling capacity of chitosan glutamate microparticles, surprisingly a higher amount of CF did not impact the time required for 80% of the drug to be released markedly. The formulation with the lowest polymer:CF ratio, 3:1, was selected as optimal, providing satisfactory drug loading and displaying a moderate burst effect within the first 30 min of the study, followed with a prolonged drug release of up to 210 min.

Insight into approximations for drug release from polymer matrix

AIChE Journal ◽  
2008 ◽  
Vol 54 (8) ◽  
pp. 2220-2227 ◽  
Author(s):  
Sung‐Hwa Lin
Keyword(s):  
Drug Release ◽  
Polymer Matrix ◽  
Insight Into

scholarly journals The ABCG2 multidrug transporter is a pump gated by a valve and an extracellular lid

2019 ◽  
Vol 10 (1) ◽  
Author(s):  
Narakorn Khunweeraphong ◽  
Daniel Szöllősi ◽  
Thomas Stockner ◽  
Karl Kuchler
Keyword(s):  
Drug Release ◽  
Molecular Mechanism ◽  
Salt Bridge ◽  
Multidrug Transporter ◽  
Peristaltic Pump ◽  
Disulfide Bridges ◽  
Control Drug ◽  
Atp Binding Cassette Transporter ◽  
Extracellular Loops ◽  
Control Drug Release

AbstractThe human ATP-binding cassette transporter ABCG2 is a key to anticancer resistance and physiological detoxification. However, the molecular mechanism of substrate transport remains enigmatic. A hydrophobic di-leucine motif in the ABCG2 core separates a large intracellular cavity from a smaller upper cavity. We show that the di-leucine motif acts as a valve that controls drug extrusion. Moreover, the extracellular structure engages the re-entry helix and all extracellular loops to form a roof architecture on top of the upper cavity. Disulfide bridges and a salt bridge limit roof flexibility, but provide a lid-like function to control drug release. We propose that drug translocation from the central to the upper cavities through the valve is driven by a squeezing motion, suggesting that ABCG2 operates similar to a peristaltic pump. Finally, the roof contains essential residues, offering therapeutic options to block ABCG2 by either targeting the valve or essential residues in the roof.

scholarly journals Antioxidant Traits of Some Nanocarbon Moieties Integrated in Polymer Materials (a Review)

2016 ◽  
Vol 10 (4s) ◽  
pp. 581-586 ◽  
Author(s):  
Eldar Zeynalov ◽  
◽  
Manfred Wagner ◽  
Joerg Friedrich ◽  
Matanat Magerramova ◽  
...  
Keyword(s):  
Mechanical Properties ◽  
Carbon Nanotubes ◽  
Polymer Matrix ◽  
Polymeric Composites ◽  
Polymer Materials ◽  
Thermal And Mechanical Properties ◽  
Fullerene Soot ◽  
The Status

This review briefly gives the status of worldwide researches in the aspect of an impact of incorporated fullerenes and carbon nanotubes (CNTs) on durability of different polymeric composites under stressful harsh therm-oxidative conditions. It has been inferred that among various nanoparticulates, fullerenes and CNTs are preferable to be used for enhancing thermal and mechanical properties of polymers. Fullerenes C60, C70, fullerene soot and CNTs being integrated in polymer matrix effectively prevent both their thermal and thermoxidative degradation, and photooxidation processes as well.

scholarly journals FORMULATION AND EVALUATION OF TOPICAL GEL OF ACYCLOVIR FOR TREATMENT OF VIRAL DISEASE

2019 ◽  
Vol 8 (6) ◽  
Author(s):  
Vivek Jatwa ◽  
M.K. Gupta ◽  
Neetesh K Jain ◽  
Urvashi Sharma ◽  
Rahul Sisodiya
Keyword(s):  
Drug Release ◽  
Research Work ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Viral Disease ◽  
Pharmacokinetic Data ◽  
Permeation Enhancer ◽  
Topical Gel ◽  
Carbopol 940

Aim: Formulation & Evaluation of Topical Gel of Acyclovir for Treatment of Viral Disease. Material & Methods: Acyclovir gels were formulated using different polymers like Carbopol 934, Carbopol 940, hydroxy propyl methyl cellulose and Sodium Carboxy methyl cellulose. Different concentrations of polymer were used in the formulation of gels. All the formulations were evaluated for the various parameters. Results & Discussion: Different formulations with use of different polymers were prepared. The amount and percentage of drug present in gel formulation using different polymers were estimated as per the procedure. The prepared gel using 1% carbopol- 934(A2) showed maximum drug content (101.72%) compared to other formulations. The spreadability of gels was determined as per the procedure. From spreadability data is observed that the formulation with 1.0% carbopol-934 showed maximum (8cm), where as the formulations with 1% carbopol-940, 3%, HPMC and Sodium CMC 3% were showed significant spreadability. 1.0 % carbopol-934 shows maximum release (74.59%). The addition of DMSO as permeation enhancer improves the drug release from gel formulation. 1.0% carbopol-940 also showed a similar release pattern, but the release was lesser. In case of HPMC and Sodium CMC gels the release was much lesser than carbopol gels. The addition of DMSO as permeation enhancer drug release was improved. Stability study for the best formulation was done as per the procedure. The gel was both physically and chemically stable at 4-50C, Room temperature and 37±50C. Conclusion: From this investigation, it was concluded that formulation A2 with 1% Carbopol-934 may be the best formulation having good in vitro release profile, stability and bioavailability. Based on the results from the study further utility of the dosage form may depend on pharmacokinetic data. Forthcoming research work of antiviral activity may contribute in the challenging area. Keywords: Acyclovir, Topical gel, Viral Disease, Skin Disease, Formulation & Development

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