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1.
J Drug Target ; 32(6): 655-671, 2024 Jul.
Article in English | MEDLINE | ID: mdl-38652465

ABSTRACT

Oral route of drug administration is typically the initial option for drug administration because it is both practical and affordable. However, major drawback of this route includes the release of drug at a specified place thus reduces the bioavailability. This could be overcome by utilising the gastroretentive drug delivery system (GRRDS). Prolonged stomach retention improves bioavailability and increases solubility for medicines that are unable to dissolve in high pH environments. Many recent advancements in the floating, bio adhesive, magnetic, expandable, raft forming and ion exchange systems have been made that had led towards advanced form of drug delivery. From the past few years, floating drug delivery system has been most commonly utilised for the delivery of drug in a delayed manner. Various polymers have been utilised for manufacturing of these systems, including alginates, chitosan, pectin, carrageenan's, xanthan gum, hydroxypropyl cellulose, carbomer, polyethylene oxide and sodium carboxy methyl cellulose. Chitosan, pectin and xanthan gum have been found to be most commonly used polymers in the manufacturing of drug inclusion complex for gastroretentive drug delivery. This study aimed to define various types and advanced polymers as well as also highlights recent advances and future perspectives of gastroretentive drug delivery system.


Subject(s)
Drug Delivery Systems , Polymers , Polymers/chemistry , Humans , Biological Availability , Administration, Oral , Solubility , Delayed-Action Preparations , Animals
2.
Drug Des Devel Ther ; 14: 2435-2448, 2020.
Article in English | MEDLINE | ID: mdl-32606610

ABSTRACT

BACKGROUND: Severe bleeding and perforation of the colon and rectum are complications of ulcerative colitis which can be treated by a targeted drug delivery system. PURPOSE: Development of colon-targeted delivery usually involves a complex formulation process and coating steps of pH-sensitive methacrylic acid based Eudragit®. The current work was purposefully designed to develop dicalcium phosphate (DCP) facilitated with Eudragit-S100-based pH-dependent, uncoated mesalamine matrix tablets. MATERIALS AND METHODS: Mesalamine formulations were compressed using wet granulation technique with varying compositions of dicalcium phosphate (DCP) and Eudragit-S100. The developed formulations were characterized for physicochemical and drug release profiles. Infrared studies were carried out to ensure that there was no interaction between active ingredients and excipients. Artificial neural network (ANN) was used for the optimization of final DCP-Eudragit-S100 complex and the experimental data were employed to train a multi-layer perception (MLP) using quick propagation (QP) training algorithm until a satisfactory root mean square error (RMSE) was reached. The ANN-aided optimized formulation was compared with commercially available Masacol®. RESULTS: Compressed tablets met the desirability criteria in terms of thickness, hardness, weight variation, friability, and content uniformity, ie, 5.34 mm, 7.7 kg/cm2, 585±5 mg (%), 0.44%, and 103%, respectively. In-vitro dissolution study of commercially available mesalamine and optimized formulation was carried out and the former showed 100% release at 6 h while the latter released only 12.09% after 2 h and 72.96% after 12 h which was fitted to Weibull release model with b value of 1.3, indicating a complex release mechanism. CONCLUSION: DCP-Eudragit-S100 blend was found explicative for mesalamine release without coating in gastric and colonic regions. This combination may provide a better control of ulcerative colitis.


Subject(s)
Neural Networks, Computer , Polymethacrylic Acids/chemistry , Tablets/chemistry , Calcium Phosphates/chemical synthesis , Calcium Phosphates/chemistry , Drug Compounding , Hydrogen-Ion Concentration , Polymethacrylic Acids/chemical synthesis , Tablets/chemical synthesis
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