Development of niosomes for encapsulating captopril-quercetin prodrug to combat hypertension.

Autor: Sayyad N; Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal (Westville Campus), Private Bag X54001, Durban 4000, South Africa., Maji R; Department of Pharmaceutics, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu Natal, (Westville Campus), Private Bag X54001, Durban, South Africa., Omolo CA; Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal (Westville Campus), Private Bag X54001, Durban 4000, South Africa; United States International University-Africa, School of Pharmacy and Health Sciences, Department of Pharmaceutics, P.O. Box 14634-00800, Nairobi, Kenya., Ganai AM; Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal (Westville Campus), Private Bag X54001, Durban 4000, South Africa., Ibrahim UH; Department of Pharmaceutics, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu Natal, (Westville Campus), Private Bag X54001, Durban, South Africa., Pathan TK; Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal (Westville Campus), Private Bag X54001, Durban 4000, South Africa., Devnarain N; Department of Pharmaceutics, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu Natal, (Westville Campus), Private Bag X54001, Durban, South Africa., Karpoormath R; Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal (Westville Campus), Private Bag X54001, Durban 4000, South Africa. Electronic address: karpoormath@ukzn.ac.za., Dhawan S; Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal (Westville Campus), Private Bag X54001, Durban 4000, South Africa., Obakachi VA; Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal (Westville Campus), Private Bag X54001, Durban 4000, South Africa., Merugu SR; Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal (Westville Campus), Private Bag X54001, Durban 4000, South Africa., Kayamba F; Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal (Westville Campus), Private Bag X54001, Durban 4000, South Africa., Mahlalela M; Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal (Westville Campus), Private Bag X54001, Durban 4000, South Africa., Govender T; Department of Pharmaceutics, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu Natal, (Westville Campus), Private Bag X54001, Durban, South Africa., Tzakos AG; Section of Organic Chemistry and Biochemistry, Department of Chemistry, University of Ioannina, Ioannina 45110, Greece., Singh S; Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal (Westville Campus), Private Bag X54001, Durban 4000, South Africa.
Jazyk: angličtina
Zdroj: International journal of pharmaceutics [Int J Pharm] 2021 Nov 20; Vol. 609, pp. 121191. Date of Electronic Publication: 2021 Oct 17.
DOI: 10.1016/j.ijpharm.2021.121191
Abstrakt: Novel and effective anti-hypertensive agents are required to manage hypertension; therefore, we synthesised a novel antihypertensive drug from captopril and quercetin (cap-que) and explored its antihypertensive potential in a niosomal formulation via molecular hybridisation. The cap-que hybrid was synthesised, and its structure was characterised via NMR, FTIR, and HRMS. Niosomes were then loaded with cap-que using the thin-film hydration method. The particle size, polydispersity index, surface charge and drug entrapment efficiency (EE%) of the formulation were 418.8 ± 4.21 nm, 0.393 ± 0.063, 16.25 ± 0.21 mV, and 87.74 ± 2.82%, respectively. The drug release profile showed a sustained release of the active compound (43 ± 0.09%) from the niosomal formulation, compared to the parent drug (80.7 ± 4.68%), over 24 h. The cell viability study confirmed the biosafety of the formulation. The in vivo study in a rat model showed enhanced antihypertensive activity of the hybrid molecule and niosomal formulation which reduced systolic and diastolic pressure when compared to the individual, bare drugs. The findings of this study concluded that the antihypertensive potential of captopril can be enhanced by its hybridisation with quercetin, followed by niosomal nano drug delivery.
(Copyright © 2021 Elsevier B.V. All rights reserved.)
Databáze: MEDLINE
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