Formulation Development, Characterization, and Evaluation of a Novel Dexibuprofen-Capsaicin Skin Emulgel with Improved I
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Research Article Formulation Development, Characterization, and Evaluation of a Novel Dexibuprofen-Capsaicin Skin Emulgel with Improved In Vivo Anti-inflammatory and Analgesic Effects Imran Khan Burki,1 Muhammad Khalid Khan,1,5 Barkat Ali Khan,1 Bushra Uzair,2 Valdir A. Braga,3 and Qazi Adnan Jamil4
Received 4 May 2020; accepted 11 July 2020 Abstract. Transdermal application of analgesics allows efficient and painless delivery of medication with minimum side effect. This study was designed with the aim to formulate and characterize dexibuprofen-capsaicin emulgel for transdermal drug delivery with improved antiinflammatory and analgesic effects. The emulgel was prepared and evaluated for physical examination, stability, spreadability, rheological behavior, viscosity, drug content determination, FTIR analysis, and ex vivo studies. Anti-inflammatory (carrageenan-induced paw edema) and analgesic (hot plate latency test) effects were determined in Sprague-Dawley rats. The dexibuprofen-capsaicin emulgel showed good physical appearance and stability having average pH 5.5 to 6.0, conductivity 73–76 s/m, spreadability (12–)17 g cm/s, drug content 102.84% ± 0.53 (for capsaicin) and 94.09% ± 0.41 (for dexibuprofen), and FTIR compatibility. It was noted that 86.956% ± 1.46 (with 100 mg menthol), 76.687% ± 1.21 (75 mg menthol), and 65.543% ± 1.71 (without menthol) of capsaicin were released. Similarly 81.342% ± 1.21 (with 100 mg menthol), 72.321% ± 1.31 (75 mg menthol), and 52.462% ± 1.23 (without menthol) of dexibuprofen were released. The cumulative amount of capsaicin permeated through rabbit skin was 9.83 ± 0.037 μg/ cm2 with 100 mg menthol (as permeation enhancer), 7.23 ± 0.037 μg/cm2 with 75 mg menthol, and 2.23 ± 0.061 μg/cm2 without menthol after 6.5 h. The permeation of dexibuprofen was 19.53 ± 0.054 μg/cm2, 13.87 ± 0.032 μg/cm2, and 3.83 ± 0.074 μg/cm2. Carrageenan-induced paw edema of rat was effectively inhibited by the optimized emulgel. Similarly it was observed that DCE5 shows higher analgesic activity compared with marketed diclofenac sodium emulgel (Dicloran®). The conclusion of this research study evidently indicated a promising synergistic potential of dexibuprofen-capsaicin emulgel as an alternative to the conventional topical dosage form. KEY WORDS: transdermal drug delivery; emulgel; capsaicin; dexibuprofen; anti-inflammatory; analgesic.
INTRODUCTION A growing numbers of drug delivery methods have been developed for drug products having low permeability, poor 1
Department of Pharmaceutics, Faculty of Pharmacy, Gomal University, D.I.Khan, Pakistan. 2 Department of Biotechnology and Bioinformatics, International Islamic University, Islamabad, Pakistan. 3 Center of Biotechnology, Federal University of Paraiba, João Pessoa, Brazil. 4 Faculty of Pharmacy and Alternative Medicine, Islamia University of Bahawalpur, Bahawalpur, Pakistan. 5 To whom correspondence should be addressed. (e–mail: [email protected]) Abbreviations: DCE5, Dexibuprofen-capsaicin emulgel; FTIR, Fourier transform infrared spectroscopy;
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