Azarbayjani, A.F and Khu, J.V and Chan, Y.W and Chan, S.Y (2011) Development and characterization of skin permeation retardants and enhancers: A comparative study of levothyroxine-loaded PNIPAM, PLA, PLGA and EC microparticles. Biopharmaceutics and Drug Disposition, 32 (7). pp. 380-388.
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Abstract
Polymeric microparticles suitable for topical and transdermal delivery systems
were studied using poly D,L lactide (PLA), poly D,L lactide co glycoside (PLGA), poly
(N-isopropylacrylamide) (PNIPAM) and ethyl cellulose (EC). Drug encapsulation efficacy, microparticle
stability and skin permeation studies of levothyroxine loaded microparticles were
carried out using excised human skin, and the skin permeation pattern was observed using
confocal laser scanning microscopy.
It was found that ethyl cellulose microparticles had the highest drug encapsulation and minimal
drug leakage during the 14week storage period. The PNIPAM microparticles had the lowest
drug encapsulation efficiency and a fast degradation rate. The PLGA microparticles exhibited a
temperature dependent drug leakage. Permeation studies using a flow-through diffusion cell
indicated that the polymer transition temperature (Tg) may influence the skin permeation rate
of levothyroxine. Polyesters (PLA and PLGA) and PNIPAM acted as a skin penetration retardant
and caused skin accumulation of the drug. These microparticles have potential use in skin
formulations containing sunscreens and other active ingredients that are meant to be
concentrated on the skin surface. However, skin permeation was observed from EC
microparticles, therefore such polymers may be used as carriers in transdermal formulations
to help achieve therapeutic concentrations of the drug in the plasma. Copyright © 2011 John
Wiley & Sons, Ltd
Item Type: | Article |
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Additional Information: | cited By 6 |
Uncontrolled Keywords: | penetration enhancers; penetration retardants; ethyl cellulose; poly D, L lactide; poly (N-isopropylacrylamide) |
Subjects: | R Medicine > R Medicine (General) |
Depositing User: | Unnamed user with email gholipour.s@umsu.ac.ir |
Date Deposited: | 12 Aug 2017 05:28 |
Last Modified: | 23 Jul 2019 06:38 |
URI: | https://eprints.umsu.ac.ir/id/eprint/1094 |