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Published on:May 2020
Indian Journal of Pharmaceutical Education and Research, 2020; 54(2s):s200-s209
Original Article | doi:10.5530/ijper.54.2s.76

Formulation and in-vitro Evaluation of Oral Captopril Bioadhesive Delivery System

Authors and affiliation (s):

Mohamed Dawoud1,2,*, Fahima Hashem2

1Department of Pharmaceutics, Faculty of Pharmacy, Umm Al Qura, University, Holy Makkah, KSA.

2Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Helwan-University, Cairo, EGYPT.


Background: Captopril is considered as the drug of choice in the treatment of hypertension and congestive heart failure. It has a very short duration of action and a biological half-life of 1-2 hr. This requires its administration in 2-3 times daily which is not convenient for the management of a chronic disease like hypertension. Objectives: Captopril is unstable at the alkaline pH of the gastrointestinal tract. Therefore, it is difficult to be delivered orally in a sustained release formulation. This defect can be overcome by using bioadhesive or floating delivery systems which could increase the residence time of the drug in the stomach. Methods: Different formulations of bioadhesive chitosan microspheres containing captopril were prepared using the cross-linking method. Characterization of these microspheres was performed by measuring percent yield, particle size, swelling and bioadhesive properties, drug content and in-vitro release of captopril. Results: Chitosan microspheres prepared from 2% high molecular weight chitosan in acetic acid with 5ml glutaraldehyde and a cross-linking time of 3 hr gave the highest yield percent (83%), the highest entrapment efficiency (55%) and sustained release over 8 hr, compared with other examined formulations of chitosan. The release kinetics from all the prepared microspheres were diffusion-controlled mechanism and the drug release from microspheres was dependent on its concentration. Conclusion: In conclusion, chitosan microspheres with their particle size and release behavior seem to be a good carrier for captopril.

Key words: Chitosan, Microspheres, Bioadhesion, Captopril, In-vitro release.



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The Official Journal of Association of Pharmaceutical Teachers of India (APTI)
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Indian Journal of Pharmaceutical Education and Research (IJPER) [ISSN-0019-5464] is the official journal of Association of Pharmaceutical Teachers of India (APTI) and is being published since 1967.


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