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Microemulsion Transdermal Formulation for Simultaneous Delivery of Valsartan and Nifedipine: Formulation by Design
Jatin Sood1, Bharti Sapra1, Ashok K Tiwary2
1Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala, 147002, India.
AAPS Pharmscitech
|November 19, 2016
Summary
This study optimized oil-in-water microemulsions for transdermal delivery of antihypertensive drugs valsartan and nifedipine. Optimized formulations significantly enhanced drug solubility and skin permeation.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Formulation Development
Background:
- Simultaneous transdermal delivery of poorly soluble antihypertensive drugs presents formulation challenges.
- Microemulsions offer potential for enhancing solubility and skin permeation of hydrophobic drugs.
Purpose of the Study:
- To optimize the composition of oil-in-water microemulsions for the co-delivery of valsartan and nifedipine.
- To investigate the impact of Captex 500, Capmul MCM, and Acrysol EL 135 on microemulsion characteristics and drug solubility.
Main Methods:
- Box-Behnken design (a response surface methodology) was employed to optimize formulation components.
- Analysis of Variance (ANOVA) was used to identify significant factors affecting particle size and drug solubility.
- Permeation studies across rat skin were conducted to evaluate drug transport.
Main Results:
- Formulation components significantly influenced microemulsion particle size and drug solubility.
- Capmul MCM and Acrysol EL 135 decreased particle size, while Captex 500 increased it.
- Optimized microemulsions achieved significant enhancement ratios for valsartan (27.21-fold) and nifedipine (63.57-fold) permeation.
Conclusions:
- Microemulsion systems are effective for solubilizing poorly soluble antihypertensive drugs.
- Optimized microemulsions enhance the transdermal transport of valsartan and nifedipine across rat skin.
- This formulation approach shows promise for combined antihypertensive therapy.
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