Abstract
Objective: The objective of the present work is to formulate and evaluate Bosentan controlled-release microcapsules using gum karaya and polyethylene oxide as polymers, sodium alginate and calcium chloride as encapsulating material and cross-linking agent and croscarmellose sodium as superdisintegrant. Methods: Bosentan microcapsules were prepared by the ionic gelation method. The prepared microcapsules were characterized by flow properties such as angle of repose, compressibility index, particle size and encapsulation efficiency and drug release profiles. Results: The prepared microcapsules were evaluated for angle of repose, compressibility index, % drug content, encapsulation efficiency and particle size. All the flow properties were within the specified IP limits. The drug content of microcapsules prepared by ionic gelation method by varying the polymeric concentration was found in the range of 121.62±0.41 to 124.99±0.51 mg. The encapsulation efficiency of Bosentan controlled-release microcapsules was found to be in the range of 59 % to 67%. Among all the formulations prepared, formulation B14 containing equal proportions (25 mg) of gum karaya and polyethylene oxide showed about 95% of drug release over a period of 12 h and were found to be suitable for extending drug release up to 16 h. Conclusion: Bosentan controlled-release microcapsules were prepared by ionic gelation method, which is a novel formulation that is helpful in the treatment of pulmonary artery hypertension (PAH).
Highlights
Controlled drug delivery system is mainly focused on to achieve passable and increased bioavailability [1]
Bosentan controlled-release microcapsules were prepared by ionic gelation method
Gum karaya and polyethylene oxide were used as controlled release coating polymeric material for the preparation of microcapsules
Summary
Controlled drug delivery system is mainly focused on to achieve passable and increased bioavailability [1]. Carrier drug delivery systems are available such as microcapsules, microspheres, nanoparticles, nanosomes, phytosomes, niosomes are available, and among these we selected one such carrier system is using microcapsules as carriers for drugs These carrier systems are greatly used to mask the taste and odor of the drug molecules, prolong the drug release, stability of drug molecules and to enhance the bioavailability [2-4]. Microencapsulation is defined as the applications of a thin polymeric coating solution to core materials are having particle size range between 5 and 5000 μm [5, 6]. It is the widely used method which extends the duration of drug action and improves patient compliance. The total dose and adverse reactions may be decreased since a steady plasma concentration is maintained [7, 8]
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