270620

Liquid and Solid Self-Emulsifying Drug Delivery Systems to Improve Dissolution of Carvedilol

Article

Last updated: 04 Jan 2025

Subjects

-

Tags

Pharmaceutics, biopharmaceutics and pharmacokinetics.

Abstract

Carvedilol has poor oral bioavailability which is attributed to its limited aqueous solubility, intestinal efflux, and pre-systemic hepatic metabolism. This work aimed to increase carvedilol bioavailability via a self-emulsifying drug delivery system (SEDDS). Liquid-SEDDS were initially prepared and the best formula with the highest drug release was converted into powder form to improve stability. A ternary phase diagram was performed using various ratios of Olive oil, Tween 80, and Propylene Glycol (as oil, surfactant, and co-solvent, respectively) to obtain 21 formulations. All formulations were characterized by visual inspection, accelerated aging, emulsification time and precipitation assessment, and in vitro drug dissolution studies. The best SEDDS formula was adsorbed onto a carrier to be transformed into solid powder, Fumed Silica, Avicel PH101, and their combinations, to obtain solid-SEDDS. Drug dissolution, DSC, and ray diffraction were performed to formula showing the best flow properties. All SEDDS showed enhanced drug dissolution relative to the pure drug, with high initial drug release. Formula F14 showed a prompt drug of about 92% within 5 minutes with a percentage dissolution efficiency of 93% after ten minutes. Formulas prepared using Avicel PH101 showed the best flow properties and were used for further investigations. Drug dissolution parameters were best from solid-SEDDS using Avicel PH101 alone. For DSC and X-ray diffraction studies, the drug characteristic peaks disappeared indicating a reduction in drug crystallinity. Solid-SEDDS could enhance the Carvedilol dissolution rate with subsequent improved oral bioavailability by decreasing its pre-systemic metabolism.

DOI

10.21608/jampr.2022.165325.1047

Keywords

Carvedilol, Dissolution, Self-emulsifying drug delivery system

Authors

First Name

Doaa

Last Name

Habib

MiddleName

A

Affiliation

Department of pharmaceutics, Faculty of pharmacy, Damanhour university, Damanhour, Egypt

Email

doaa.habib@pharm.dmu.edu.eg

City

-

Orcid

0000-0002-8780-5842

First Name

Heba

Last Name

Elbedaiwy

MiddleName

M

Affiliation

Department of Pharmaceutics, Faculty of Pharmacy, Damanhour University, Damanhour, Egypt

Email

heba.elbedaiwy@pharm.dmu.edu.eg

City

-

Orcid

-

First Name

Ebtessam

Last Name

Essa

MiddleName

A

Affiliation

Department of Pharmaceutical Technology, Faculty of Pharmacy, Tanta University, Tanta, Egypt

Email

ebtesam.eisa@pharm.tanta.edu.eg

City

-

Orcid

-

Volume

4

Article Issue

1

Related Issue

40423

Issue Date

2023-03-01

Receive Date

2022-09-27

Publish Date

2023-03-01

Page Start

1

Page End

10

Online ISSN

2636-4158

Link

https://jampr.journals.ekb.eg/article_270620.html

Detail API

https://jampr.journals.ekb.eg/service?article_code=270620

Order

270,620

Type

Original Article

Type Code

855

Publication Type

Journal

Publication Title

Journal of Advanced Medical and Pharmaceutical Research

Publication Link

https://jampr.journals.ekb.eg/

MainTitle

Liquid and Solid Self-Emulsifying Drug Delivery Systems to Improve Dissolution of Carvedilol

Details

Type

Article

Created At

24 Dec 2024