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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
- Source :
- AAPS PharmSciTech. 21
- Publication Year :
- 2020
- Publisher :
- Springer Science and Business Media LLC, 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 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.
- Subjects :
- Male
medicine.drug_class
Skin Absorption
Analgesic
Pharmaceutical Science
Ibuprofen
02 engineering and technology
Aquatic Science
Pharmacology
Administration, Cutaneous
Carrageenan
030226 pharmacology & pharmacy
Anti-inflammatory
Dexibuprofen
Rats, Sprague-Dawley
03 medical and health sciences
chemistry.chemical_compound
0302 clinical medicine
In vivo
Drug Discovery
medicine
Animals
Edema
Ecology, Evolution, Behavior and Systematics
Skin
Transdermal
Analgesics
Ecology
Viscosity
Chemistry
Anti-Inflammatory Agents, Non-Steroidal
General Medicine
Diclofenac Sodium
021001 nanoscience & nanotechnology
Rats
Capsaicin
Emulsions
Rabbits
0210 nano-technology
Menthol
Gels
Agronomy and Crop Science
medicine.drug
Subjects
Details
- ISSN :
- 15309932
- Volume :
- 21
- Database :
- OpenAIRE
- Journal :
- AAPS PharmSciTech
- Accession number :
- edsair.doi.dedup.....33af94f3729e5d5c540c0e69fd1189e3
- Full Text :
- https://doi.org/10.1208/s12249-020-01760-7