FABRICATION AND EVALUATION OF ORAL CONTROLLED RELEASE OF MUCOADHESIVE ALGINATE MICROBEADS CONTAINING FLUVASTATIN SODIUM
Objective: The aim of this study is to prepare oral controlled release (CR) of mucoadhesive alginate microbeads encapsulating fluvastatin by gastroretention technology.
Methods: The mucoadhesive microbeads containing fluvastatin were produced using emulsification internal gelation technique. The effect of different variables such as sodium alginate concentration and its combination with other hydrophilic polymers, and the effect of various curing agents on particle size, entrapment efficiency, and in vitro studies were evaluated.
Results: There was no marked change in drug entrapment efficiency, and dissolution studies occur during the stability studies of fluvastatin. The in vitro results give data that improvement in the CR of the drug from microbeads compared with marketed tablet. Hence, in this regard, to minimize the frequency of drug administration to reduce side effects. The optimum condition for the preparation of stable alginate beads and produce CR manner was occurred at a higher concentration of combined polymer mixture in equal ratios, i.e., 3% w/v. Infrared spectroscopic study (Fourier transform infrared) confirmed the no incompatibility between drug and other excipients. X-ray diffraction study and differential scanning calorimetry were provided evidence that successful entrapment of drug into the alginates microbeads and drug converted into amorphous nature. The efficiency of mucoadhesion strength of microbeads was determined by wash-off study.
Conclusion: The kinetic modeling of the release data indicates drug release from the microbeads follow anomalous transport mechanism and super Case-II transport mechanism. Drug release is a function of pH dependent and controlled drug release depends on type and concentration of polymer blend and curing agents. The release kinetics of drug from the alginate beads followed zero order.
2. Arora S, Ali J, Ahuja A, Khar RK, Baboota S. Floating drug delivery systems: A review. AAPS PharmSciTech 2005;6:E372-90.
3. Chien YW, Shoufeng Li, Lin S, Daggy BP. Effect of formulation variables on the floating properties of gastric floating drug delivery system. Drug DevInd Pharm 2002;28:783-79.
4. Toda T, Eliasson E, Ask B, Inotsume N, Rane A. Roles of different CYP enzymes in the formation of specific fluvastatin metabolites by human liver microsomes. Basic ClinPharmacolToxicol 2009;105:327-32.
5. Sirbu C, Tomuta I, Achim M, Rus LL, Vonica L, Dinte E. Quantitative characterization of powder blends for tablets with indapamide by near infrared spectroscopy and chemometry. Farmacia 2014;62:48-57.
6. Funami T, Fang Y, Noda S, Ishihara S. Nakauma M, Draget KI, et al. Rheological properties of sodium alginate in an aqueous system during gelation in relation to super molecular structures and Ca2+ binding. Food Hydrocoll 2009;23:1746-55.
7. Tokumura T, Machida Y. Preparation of amoxicillin intragastric buoyant sustained-release tablets and the dissolution characteristics. J Control Release 2006;110:581-6.
8. Chavanpatil MD, Jain P, Chaudhari S, Shear R, Vavia PR. Novel sustained release, swellable and bioadhesivegastroretentive drug delivery system for ofloxacin. Int J Pharm 2006;316:86-92.
9. Nur AO, Zhang JS. Captopril floating and/or bioadhesive tablets: Design and release kinetics. Drug DevInd Pharm 2000;26:965-9.
10. Piyakulawat P, Praphairaksit N, Chantarasiri N, Muangsin N. Preparation and evaluation of chitosan/carrageenan beads for controlled release of sodium diclofenac. AAPS PharmSciTech 2007;8:E97.
11. Reddy KV, Nagabhushanam MV. The role of needle in formulation of pH sensitive swellable microbeads prepared with hydrophilic polymers for atorvastatin and their characterization studies. Int J App Pharm 2017;9:20-30.
12. Peppas NA. Analysis of fickian and non-fickian drug release from polymers. Pharm ActaHelv 1985;60:110-1.
13. Pawar S. Formulation and evaluation of garlic powder loaded floating matrix tablet. Int J Pharm PharmSci 2019;11:17-21.
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