Formulation and in-vitro Evaluation of Oral Captopril Bioadhesive Delivery System
1,2, 2
- 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.
CORRESPONDENCE
Mohamed Dawoud
Department of Pharmaceutics, Faculty of Pharmacy, Umm Al Qura, University, Holy Makkah, KSA.
Received: 19-11-2019; Accepted: 30-04-2020.
Volume 54, Issue 2s (Supplement) · pp. s200-s209 · 2020 · DOI: 10.5530/ijper.54.2s.76
ABSTRACT
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.
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Dawoud, M., & Hashem, F. (2020). Formulation and in-vitro Evaluation of Oral Captopril Bioadhesive Delivery System. Indian Journal of Pharmaceutical Education and Research, 54(2s), s200-s209. https://doi.org/10.5530/ijper.54.2s.76
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