Abstract
Objective: The aim of the present work was to prepare and examine drug release of the oral controlled release microbeads using different curing agents by emulsification internal ionic gelation technique.
 Methods: Cross-linked alginate microbeads were prepared with different cross linking agents by using mucoadhesive properties. The formation and compatibility of microbeads were confirmed by compatibility studies. Prepared microbeads evaluated for encapsulated efficiency, micromeritic properties, drug loading, in vitro wash off studies, in vitro dissolution studies, drug release kinetics and stability studies
 Results: The in vitro drug release was influenced by both type of curing agents and type of polymers and no significant changes in characterization parameters was observed after 3 mo stability studies. The sustained release profile of optimized batch was found to be 99.66±0.18% in comparison to pure drug profile of 28.64±0.02% at 12 h release study. Results of both wash-off and in vitro studies suggests that batch (SF2) prepared with aluminium chloride has shown better mucoadhesive property. Drug release of optimized batch follows zero order with non fickian mechanism according to Korsmeyer-Peppas equation.
 Conclusion: The data suggest the use of simvastatin mucoadhesive cross linked microbeads to offer the potential for oral controlled drug delivery with improved gastric retention and capable to provide sustained drug release by using cross linking agents.
Highlights
Gastroretentive systems can remain in the gastric cavity for several hours and prolong the gastric residence time of drugs, maximum utilization of drug
The main aim of Gastro-retentive drug delivery systems (GRDDS) which prolongs the gastric residence time of the formulations by forming strong intimate contact, improves solubility for drugs that are less soluble in a high pH environment and prolonged gastric retention improves bioavailability and therapeutic efficacy, reduced frequency of drug administration, reduction in dose size, improved patient compliance and/or to achieve a local effect in the stomach [1]
Simvastatin is used in treatment of hyperlipidemic patients and available in crystalline state with hygroscopic nature and belongs to BCS class II drug with a half-life of less than 3 h and bioavailability of less than 5% as its limited by absorption rate factor [4]
Summary
Gastroretentive systems can remain in the gastric cavity for several hours and prolong the gastric residence time of drugs, maximum utilization of drug. Simvastatin is used in treatment of hyperlipidemic patients and available in crystalline state with hygroscopic nature and belongs to BCS class II drug with a half-life of less than 3 h and bioavailability of less than 5% as its limited by absorption rate factor [4]. It often shows dissolution rate-limited oral absorption. Multiparticulate systems avoid the vagaries of gastric emptying and different transit rates; thereby release the drugs more uniformly [6]
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