Formulation study of a patch containing propranolol by design of experiments.
Francesco Cilurzo1, Paola Minghetti, Chiara G M Gennari
1Department of Pharmaceutical Sciences, Università degli Studi di Milano , Milan , Italy.
Drug Development and Industrial Pharmacy
|January 11, 2013
Summary
This study developed a transdermal propranolol (PR) patch, finding that matrix thickness and PR content are key factors for drug diffusion. The optimized patch ensures non-irritating, constant PR delivery for 48 hours.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Dermatology
Background:
- Transdermal drug delivery offers advantages over oral administration for certain medications.
- Propranolol (PR), a beta-blocker, has potential for transdermal delivery to manage various conditions.
- Optimizing transdermal patch formulations is crucial for effective and safe drug delivery.
Purpose of the Study:
- To assess the feasibility of developing a transdermal patch for propranolol (PR) delivery.
- To identify critical formulation parameters influencing PR permeation through human skin.
- To develop a non-irritating transdermal PR patch with consistent drug release.
Main Methods:
- A quality by design approach utilizing a 2(4) full factorial design for patch development.
- Selection and evaluation of skin penetration enhancers (SPEs) for PR.
- In vitro permeation studies using Franz diffusion cells with human epidermis.
- Skin irritation assessment via the Draize test.
Main Results:
- N-methyl pyrrolidone (NMP) was identified as the most effective SPE.
- Matrix thickness and PR content significantly influenced PR flux (p<0.0957 and p<0.0004, respectively).
- Optimal formulation achieved a PR flux of 12.7 μg/cm²/h, with an estimated patch surface area of 100-120 cm².
Conclusions:
- A transdermal patch containing (S)-propranolol was successfully prepared.
- The optimized patch formulation, featuring a 50 μm methacrylic matrix with 8% (S)-PR and 15% NMP, demonstrated a flux of 13.3 μg/cm²/h.
- This formulation is non-irritating and suitable for ensuring consistent PR permeation over 48 hours, confirming the viability of transdermal PR administration.
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