Percutaneous Penetration Modifiers and Formulation Effects: Thermal and Spectral Analyses |
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Authors: | Diksha Kaushik Bozena Michniak-Kohn |
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Institution: | (1) Ernest Mario School of Pharmacy, Rutgers—The State University of New Jersey, Piscataway, New Jersey 08854, USA;(2) New Jersey Center for Biomaterials, Rutgers—The State University of New Jersey, Piscataway, New Jersey 08854, USA; |
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Abstract: | The study investigated the formulation effects of laurocapram and iminosulfurane derived penetration modifiers on human stratum
corneum using thermal and spectral analyses. Firstly, formulations of penetration modifiers were assessed as enhancers/retardants
using the model permeant, diethyl-m-toluamide followed by investigation of their mechanisms of action using differential scanning calorimetry (DSC) and attenuated
total reflectance Fourier-transform infra-red spectroscopy. The penetration modifiers investigated were laurocapram, 3-dodecanoyloxazolidin-2-one
(N-0915), S,S-dimethyl-N-(4-bromobenzoyl) iminosulfurane (DMBIS), S,S-dimethyl-N-(2-methoxycarbonylbenzenesulfonyl) iminosulfurane (DMMCBI) and tert-butyl 1-dodecyl-2-oxoazepan-3-yl-carbamate (TBDOC) that were formulated in either water, propylene glycol (PG), ethanol or
polyethylene glycol 400 (PEG 400). The results explain the mechanism for the first time why an enhancer can become a retardant
or vice versa depending upon the vehicle in which it is applied to the skin. DSC indicated that penetration modifier formulations enhanced
permeation of active mainly by disruption and fluidization of the stratum corneum lipid bilayers while IR data indicated characteristic
blue shifts with decreases in peak intensity. On the other hand, DSC of penetration modifier formulations showing retardation
depicted elevated T
m2 with a strengthening of lipid–protein complex while IR results indicated formation of multiple peaks around 1,738 cm−1 transition in stratum corneum spectra suggesting retardation may be caused by organization of SC lipids by increased H-bonding. |
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