Cited by 99Advancements in Transdermal Drug DeliveryAdvanced Drug Delivery SystemsNanoparticle-Based Drug Delivery

Oil based nanocarrier system for transdermal delivery of ropinirole: A mechanistic, pharmacokinetic and biochemical investigation

Azeem, Adnan, Talegaonkar, Sushama, Negi, Lalit M., Ahmad, Farhan J., Khar, Roop K., Iqbal, Zeenat·2012·International Journal of Pharmaceutics

Abstract

Ropinirole, a recent introduction in the clinical treatment of Parkinson's disease, suffers with the problems of low oral bioavailability and frequent dosing. An effective transdermal nano-emulsion drug delivery system can however resolve these issues effectively with greater therapeutic benefits and clinical significance. Therefore, the present work focuses precisely on pharmacokinetic, biochemical and mechanistic assessment of transdermal nanoemulsion gel in rats induced with Parkinson lesioned brain by 6-OHDA. DSC and FT-IR studies showed that NEG affects the normal lipid packing of stratum corneum to enhance the drug permeation. Study of pharmacokinetic parameters (AUC, C(max), and T(max)) revealed a greater and more extended release of ropinirole from nanoemulsion gel compared to that from a conventional gel (RPG) and oral marketed tablet (Ropitor). The AUC(0→∞) for RPCNG and RPTNG was found to be 928.07 ± 206.5 and 1055.99 ± 251.7 ngh/mL, respectively in comparison to 137.25 ± 31.3 and 467.15 ± 106.1 ngh/mL for RPG and oral tablet, respectively. The relative bioavailability of ropinirole has been enhanced more than two fold by RPTNG. Furthermore, antiparkinson activity was evaluated in terms of estimating the level of thiobarbituric acid reactive substances, glutathione antioxidant enzymes and catalase in lesioned brain of rats. Formulations were also found to be non-toxic and non-irritant by histological investigations.

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Crossref · 10.1016/j.ijpharm.2011.10.039

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  • Nanocarrier-based transdermal delivery of ropirinole restored deviated oxidative stress markers in PD rat model.

    “In another study, nanocarrier-based transdermal delivery of the DA agonist ropirinole restored deviated oxidative stress markers such as thiobarbituric acid, glutathione antioxidant enzymes and catalase in the PD rat model.125”

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Authors
Azeem, A., Talegaonkar, S., Negi, L. M., Ahmad, F. J., Khar, R. K., & Iqbal, Z.
Affiliations
  • Jubilant Life Sciences (India) (IN)
  • Jamia Hamdard (IN)
Corresponding author
Talegaonkar, Sushama
Venue
International Journal of Pharmaceutics
Publisher
Elsevier BV
Published
2012-01
Volume
422
Issue
1-2
Pages
436-444
ISSN
0378-5173 (ISSN-L)
OpenAlex
W2026763513
Cited by
99
References
36
Citations by year
2026: 3 · 2025: 6 · 2024: 7 · 2023: 6 · 2022: 7 · 2021: 9 · 2020: 9 · 2019: 10 · 2018: 5 · 2017: 7 · 2016: 7 · 2015: 4 · 2014: 5 · 2013: 11 · 2012: 3
FWCI
3.73
Type
journal article
Language
en
Open access
closed
Locations
  • International Journal of Pharmaceutics (publishedVersion)
  • PubMed (publishedVersion)
Topics
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advancements in Transdermal Drug Delivery
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
  • Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
Keywords
ropinirole, transdermal drug delivery, nanoemulsion gel, Parkinson's disease, skin permeation, pharmacokinetics, relative bioavailability, antioxidant enzymes, catalase, glutathione, TBARS
MeSH terms
Administration, Cutaneous, Administration, Oral, Animals, Antiparkinson Agents, Biological Availability, Brain, Calorimetry, Differential Scanning, Catalase, Chemistry, Pharmaceutical, Delayed-Action Preparations, Disease Models, Animal, Dihydroxyphenylalanine, Drug Carriers, Drug Compounding, Emulsions, Gels, Glutathione, Indoles, Male, Oils, Skin Absorption, Tablets, Technology, Pharmaceutical, Rats, Wistar, Thiobarbituric Acid Reactive Substances, Spectroscopy, Fourier Transform Infrared, Parkinsonian Disorders, Nanotechnology, Rats, Nanoparticles

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