Chih-Wen Fang 1 , Ling-Chun Tsai 2 , Yaw-Syan Fu 3 , Ting-Yu Cheng 2 , Pao-Chu Wu 2,4 . Show Affiliations »
Abstract
OBJECTIVE: The aim of the present study was to design nanocarriers for the topical application of rivastigmine. METHODS: The effect of cosurfactants, hydrophilic gel and loading amount on the permeability of rivastigmine through rat skin was evaluated. Skin irritation tests and stability tests were performed to evaluate the utility of tested formulations. RESULTS: The results showed that the microemulsion formation and characteristics of drug-loaded formulations were related to many parameters of the components. When using microemulsion systems as a vehicle, the permeation rate remarkably increased about 13.2~24.3-fold and the lag time was significantly shortened from 24 h to 4.7 h. Formulations containing a cosurfactant of Diethylene Glycol Monobutyl Ether (DEGBE) showed higher enhancement effect, while increasing the loading dose from 0.5% to 5% further increased the flux about 2.1-fold and shortened the lag time. CONCLUSION: The drug-loaded experimental formulation did not cause skin irritation and had good stability at 20ºC and 40ºC storage for at least 3 months. The result showed that gel-based microemulsion formulation could be a promising approach for topical administration. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.
OBJECTIVE: The aim of the present study was to design nanocarriers for the topical application of rivastigmine . METHODS: The effect of cosurfactants, hydrophilic gel and loading amount on the permeability of rivastigmine through rat skin was evaluated. Skin irritation tests and stability tests were performed to evaluate the utility of tested formulations. RESULTS: The results showed that the microemulsion formation and characteristics of drug-loaded formulations were related to many parameters of the components. When using microemulsion systems as a vehicle, the permeation rate remarkably increased about 13.2~24.3-fold and the lag time was significantly shortened from 24 h to 4.7 h. Formulations containing a cosurfactant of Diethylene Glycol Monobutyl Ether (DEGBE ) showed higher enhancement effect, while increasing the loading dose from 0.5% to 5% further increased the flux about 2.1-fold and shortened the lag time. CONCLUSION: The drug-loaded experimental formulation did not cause skin irritation and had good stability at 20ºC and 40ºC storage for at least 3 months. The result showed that gel-based microemulsion formulation could be a promising approach for topical administration. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.
Entities: Chemical
Disease
Species
Keywords:
Rivastigmine; diethylene glycol monobutyl ether; hydrophilic gel; microemulsion; skin irritation; stability.
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Year: 2020
PMID: 31729297 DOI: 10.2174/1389201020666191113144636
Source DB: PubMed Journal: Curr Pharm Biotechnol ISSN: 1389-2010 Impact factor: 2.837