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267732

Statistically-Based Optimization of Verapamil Hydrochloride Loaded Gastroretentive Alginate Beads

Article

Last updated: 03 Jan 2025

Subjects

-

Tags

Section C: Drug Design, Delivery & Targeting

Abstract

O
Objectives: A gastroretentive drug delivery system is one of many oral drug delivery systems developed to improve drug bioavailability and control drug release. It allows prolongation of drug gastric residence period for several hours. Verapamil Hydrochloride (VerHCl) is a good candidate for gastro retention because it has narrow absorption window and short half life. The goal of this study was formulation and evaluation of optimized VerHCl loaded gastroretentive alginate beads for increasing drug bioavailability and decreasing its dosing frequency. Methods: VerHCl loaded alginate beads were prepared according to 23 full factorial design using ionotropic emulsion gelation method. The effect of three formulation variables; oil concentration (%w/v) (X1), polymer concentration (%w/v) (X2) and drug to polymer ratio (X3) was investigated on mean diameter (Y1), drug loading % (Y2), entrapment efficiency (EE%) (Y3), % drug released at 1 (Y4), 5 (Y5) and 8 hr (Y6). The optimized formula was further assessed in terms of in vitro floating, in-vitro drug release, in vivo gastro retention in rats and flowability. Results: Design-Expert® numerical optimization revealed that optimum formulation levels for VerHCl loaded alginate gastroretentive beads were; oil concentration (X1) = 17.2 %w/v, polymer concentration (X2) = 4.34 %w/v and drug to polymer ratio=1.2. The optimized formula exhibited yield% (85.63± 2.65%), Drug loading% (13.60±0.89%), EE% (60.11± 2.52%), prolonged floatability with no initial lag time, sustained in vitro drug release over 8 hr, gastroretention in rats over 8 hr and good flowability. Conclusion: The optimized formula of VerHCl loaded alginate beads could be promising for retaining VerHCl in stomach for a prolonged time which could possibly be advantageous in terms of bioavailability and patient compliance.

DOI

10.21608/aprh.2022.158576.1189

Keywords

Verapamil Hydrochloride, Gastroretentive systems, bioavailability, alginate beads, Controlled drug release

Authors

First Name

Aliaa

Last Name

Ismail

MiddleName

-

Affiliation

Pharmaceutics and Industrial Pharmacy Department, Faculty of Pharmacy, Helwan University, Ain Helwan, Cairo 11795, Egypt

Email

aliaa_adly@pharm.helwan.edu.eg

City

Cairo

Orcid

0000-0002-7392-1690

First Name

Eman

Last Name

Raafat

MiddleName

-

Affiliation

Pharmaceutics and Industrial Pharmacy Department, Faculty of Pharmacy, Helwan University, Ain Helwan, Cairo 11795, Egypt

Email

emanraafat2016@gmail.com

City

Cairo

Orcid

-

First Name

Wedad

Last Name

Sakran

MiddleName

-

Affiliation

Pharmaceutics and Industrial Pharmacy Department, Faculty of Pharmacy, Helwan University, Ain Helwan, Cairo 11795, Egypt

Email

wedad_skran@pharm.helwan.edu.eg

City

cairo

Orcid

0000-0002-4880-8397

Volume

6

Article Issue

4

Related Issue

37446

Issue Date

2022-10-01

Receive Date

2022-08-25

Publish Date

2022-10-01

Page Start

207

Page End

222

Print ISSN

2357-0547

Online ISSN

2357-0539

Link

https://aprh.journals.ekb.eg/article_267732.html

Detail API

https://aprh.journals.ekb.eg/service?article_code=267732

Order

4

Type

Research Article

Type Code

318

Publication Type

Journal

Publication Title

Journal of Advanced Pharmacy Research

Publication Link

https://aprh.journals.ekb.eg/

MainTitle

Statistically-Based Optimization of Verapamil Hydrochloride Loaded Gastroretentive Alginate Beads

Details

Type

Article

Created At

22 Jan 2023