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Formulation Development, Characterization, and Evaluation of a Novel Dexibuprofen-Capsaicin Skin Emulgel with Improved In Vivo Anti-inflammatory and Analgesic Effects

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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 anti-inflammatory 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.

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Abbreviations

DCE5:

Dexibuprofen-capsaicin emulgel

FTIR:

Fourier transform infrared spectroscopy

CIPE:

Carrageenan-induced paw edema

PG:

Propylene glycol

D/W:

Distilled water

TEA:

Triethanolamine

MP:

Methyleparaben

SC:

Stratum corneum

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Acknowledgments

We are thankful to Dr. Nauman Rahim Khan (Lecturer at Faculty of Pharmacy, Gomal University, D.I.Khan Pakistan) for conducting FTIR analysis in this study.

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Authors and Affiliations

  1. Department of Pharmaceutics, Faculty of Pharmacy, Gomal University, D.I.Khan, Pakistan

    Imran Khan Burki, Muhammad Khalid Khan & Barkat Ali Khan

  2. Department of Biotechnology and Bioinformatics, International Islamic University, Islamabad, Pakistan

    Bushra Uzair

  3. Center of Biotechnology, Federal University of Paraiba, João Pessoa, Brazil

    Valdir A. Braga

  4. Faculty of Pharmacy and Alternative Medicine, Islamia University of Bahawalpur, Bahawalpur, Pakistan

    Qazi Adnan Jamil

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  1. Imran Khan Burki
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  2. Muhammad Khalid Khan
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Correspondence to Muhammad Khalid Khan.

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Conflict of Interest

The authors declare that they have no conflict of interest.

Ethics Approval and Consent to Participate

The study was approved by the Ethical Review Board of Gomal University, Dera Ismail Khan Pakistan, under reference no. ERB/GU/09-2019.

Human and Animal Rights

No human volunteers were used in this study although in vivo studies were conducted in animals which were approved by the Ethical Review Board Gomal University, Dera Ismail Khan Pakistan, under reference no. (ERB/GU/09-2019).

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Burki, I.K., Khan, M.K., Khan, B.A. et al. Formulation Development, Characterization, and Evaluation of a Novel Dexibuprofen-Capsaicin Skin Emulgel with Improved In Vivo Anti-inflammatory and Analgesic Effects. AAPS PharmSciTech 21, 211 (2020). https://doi.org/10.1208/s12249-020-01760-7

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