ABSTRACT
Purpose
The acne skin is characteristic of a relatively lower pH microenvironment compared to the healthy skin. The aim of this work was to utilize such pH discrepancy as a site-specific trigger for on-demand topical adapalene delivery.
Methods
The anti-acne agent, adapalene, was encapsulated in acid-responsive polymer (Eudragit® EPO) nanocarriers via nanoprecipitation. The nanocarriers were characterized in terms of particle size, surface morphology, drug-carrier interaction, drug release and permeation.
Results
Adapalene experienced a rapid release at pH 4.0 in contrast to that at pH 5.0 and 6.0. The permeation study using silicone membrane revealed a significant higher drug flux from the nanocarrier (6.5 ± 0.6 μg.cm−2.h−1) in comparison to that (3.9 ± 0.4 μg.cm−2.h−1) in the control vehicle (Transcutol®). The in vitro pig skin tape stripping study showed that at 24 h post dose-application the nanocarrier delivered the same amount of drug to the stratum corneum as the positive control vehicle did.
Conclusions
The acid-responsive nanocarriers hold promise for efficient adapalene delivery and thus improved acne therapy.
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Abbreviations
- ANOVA:
-
Analysis of variance
- DLS:
-
Dynamic light scattering
- FTIR:
-
Fourier transform infrared spectroscopy
- HPLC:
-
High performance liquid chromatography
- MWCO:
-
Molecular weight cut-off
- NMR:
-
Nuclear magnetic resonance
- PVA:
-
Poly(vinyl alcohol)
- SC:
-
Stratum corneum
- SDS:
-
Sodium dodecyl sulphate
- THF:
-
Tetrahydrofuran
- Transcutol®:
-
Diethylene glycol monoethyl ether
- XRD:
-
X-ray diffraction
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ACKNOWLEDGMENTS AND DISCLOSURES
The work was supported by the National Natural Science Foundation of China (81250110084; 11001197), the Tianjin Research Program of Application Foundation and Advanced Technology (13JCQNJC13300), and the Research Fund for the Doctoral Program of Higher Education of China (20110032120077). The authors of this article have no conflicts of interest to declare.
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Guo, C., Khengar, R.H., Sun, M. et al. Acid-Responsive Polymeric Nanocarriers for Topical Adapalene Delivery. Pharm Res 31, 3051–3059 (2014). https://doi.org/10.1007/s11095-014-1398-z
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DOI: https://doi.org/10.1007/s11095-014-1398-z