Appraisal of Transdermal Water-in-Oil Nanoemulgel of Selegiline HCl for the Effective Management of Parkinson’s Disease: Pharmacodynamic, Pharmacokinetic, and Biochemical Investigations
| Autor: | B. K. Razdan, Tushar Madaan, Sonal Setya, Sushama Talegaonkar, Mohammad Tariq |
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| Rok vydání: | 2017 |
| Předmět: |
Male
Skin Absorption Pharmaceutical Science 02 engineering and technology Aquatic Science Administration Cutaneous 030226 pharmacology & pharmacy Antiparkinson Agents 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Parkinsonian Disorders Pharmacokinetics Selegiline Drug Discovery Animals Rats Wistar Isopropyl myristate Ecology Evolution Behavior and Systematics Transdermal PEG 400 Chromatography Ecology Viscosity Water General Medicine Permeation 021001 nanoscience & nanotechnology Nanostructures Rats Bioavailability chemistry Distilled water Thermodynamics Emulsions Pharmaceutical Vehicles 0210 nano-technology Gels Oils Agronomy and Crop Science Selegiline Hydrochloride |
| Zdroj: | AAPS PharmSciTech. 19:573-589 |
| ISSN: | 1530-9932 |
| DOI: | 10.1208/s12249-017-0868-0 |
| Popis: | In the present study, the potential of transdermal nanoemulsion gel of selegiline hydrochloride for the treatment of Parkinson’s disease was investigated. Water-in-oil nanoemulsions were developed by comparing low- and high-energy methods and were subjected to thermodynamic stability tests, in vitro permeation, and characterization studies. In vitro studies indicated that components of nanoemulsion acted as permeation enhancers with highest flux of 3.531 ± 1.94 μg/cm2/h from nanoemulsion SB6 containing 0.5 mg selegiline hydrochloride, 3% distilled water, 21% S mix (Span 85, Tween 80, PEG 400), and 76% isopropyl myristate by weight. SB6 with the least droplet size of 183.4 ± 0.35 nm, polydispersity index of 0.42 ± 0.06 with pH of 5.9 ± 0.32 and viscosity of 22.42 ± 0.14 cps was converted to nanoemulsion gel NEGS4 (viscosity = 22,200 ± 400 cps) by addition of Viscup160® for ease of application and evaluated for permeation, safety, and pharmacokinetic profile in Wistar rats. It provided enhancement ratio 3.69 times greater than conventional gel. NEGS4 showed 6.56 and 5.53 times increase in bioavailability in comparison to tablet and conventional gel, respectively, along with sustained effect. Therefore, the developed water-in-oil nanoemulsion gel promises to be an effective vehicle for transdermal delivery of selegiline hydrochloride. |
| Databáze: | OpenAIRE |
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