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Published on: January 14, 2020
Formulation and evaluation of flurbiprofen microemulsion
K W Ambade1, S L Jadhav, M N Gambhire
1Department of Pharmaceutics, Bharati Vidyapeeth's College of Pharmacy, CBD Belapur, Sector-8, Navi-Mumbai, India.
Abstract:
The purpose of the present study was to investigate the microemulsion formulations for topical delivery of Flurbiprofen (FP) in order to by pass its gastrointestinal adverse effects. The pseudoternary phase diagrams were developed and various microemulsion formulations were prepared using Isopropyl Myristate (IPM), Ethyl Oleate (EO) as oils, Aerosol OT as surfactant and Sorbitan Monooleate as cosurfactant. The transdermal permeability of flurbiprofen from microemulsions containing IPM and EO as two different oil phases was analyzed using Keshary-Chien diffusion cell through excised rat skin. Flurbiprofen showed higher in vitro permeation from IPM as compared to that of from EO microemulsion. Thus microemulsion containing IPM as oil phase were selected for optimization. The optimization was carried out using 2(3) factorial design. The optimized formula was then subjected to in vivo anti-inflammatory study and the performance of flurbiprofen from optimized formulation was compared with that of gel cream. Flurbiprofen from optimized microemulsion formulation was found to be more effective as compared to gel cream in inhibiting the carrageenan induced rat paw edema at all time intervals. Histopathological investigation of rat skin revealed the safety of microemulsion formulation for topical use. Thus the present study indicates that, microemulsion can be a promising vehicle for the topical delivery of flurbiprofen.
Insights
This study developed microemulsions for topical Flurbiprofen (FP) delivery, bypassing gastrointestinal issues. Optimized formulations containing Isopropyl Myristate (IPM) showed superior anti-inflammatory effects and skin safety compared to gel cream.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Dermatology
Background:
- Gastrointestinal adverse effects limit oral Flurbiprofen (FP) use.
- Topical drug delivery offers an alternative route to bypass systemic side effects.
- Microemulsions present a potential vehicle for enhanced topical drug permeation.
Purpose of the Study:
- To investigate microemulsion formulations for topical Flurbiprofen (FP) delivery.
- To evaluate and optimize microemulsions for enhanced transdermal permeation and efficacy.
- To assess the safety of microemulsion formulations for topical application.
Main Methods:
- Development of pseudoternary phase diagrams for microemulsion formulation.
- Preparation of microemulsions using Isopropyl Myristate (IPM) or Ethyl Oleate (EO) as oil phases, Aerosol OT, and Sorbitan Monooleate.
- In vitro transdermal permeability studies using Keshary-Chien diffusion cells with excised rat skin.
- Optimization using a 2(3) factorial design.
- In vivo anti-inflammatory studies evaluating carrageenan-induced rat paw edema.
- Histopathological examination of rat skin.
Main Results:
- Flurbiprofen (FP) exhibited higher in vitro permeation from IPM-based microemulsions compared to EO-based ones.
- Optimized IPM microemulsions demonstrated significantly greater in vivo anti-inflammatory efficacy than a conventional gel cream.
- Histopathological analysis confirmed the safety of the microemulsion formulation for topical use.
Conclusions:
- Microemulsions containing Isopropyl Myristate (IPM) are effective vehicles for topical Flurbiprofen (FP) delivery.
- This approach successfully bypasses gastrointestinal adverse effects associated with oral FP.
- Microemulsions offer a promising and safe alternative for topical anti-inflammatory treatment.
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