Journal
INTERNATIONAL JOURNAL OF NANOMEDICINE
Volume 9, Issue -, Pages 2517-2525Publisher
DOVE MEDICAL PRESS LTD
DOI: 10.2147/IJN.S60270
Keywords
diabetic retinopathy; sustained release; ocular drug delivery; desolvation method
Funding
- Natural Science Foundation Project of CQ CSTC [cstc2012jjA10021]
- National Research Foundation for the Doctoral Program of Higher Education of China [20125503120003]
- Scientific and Technological Research Program of Chongqing Municipal Education Commission [KJ110323, KJ120307]
- Chongqing Board of Health Project [2013-2-060]
- Chongqing Yuzhong District Science and Technology Project [20100203]
- Students' Research and Innovation Experimental Project of Chongqing Medical University [201244, 201229, 201217]
- Students' Scientific Research Fund of star of HIFU [XS201309]
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This study aimed to optimize and evaluate a thermoresponsive ophthalmic in situ gel containing curcumin-loaded albumin nanoparticles (Cur-BSA-NPs-Gel). Albumin nanoparticles were prepared via a desolvation method, and the gels were prepared via a cold method. The central composite design and response surface method was used to evaluate the effects of varying Pluronic (R) F127 and Pluronic (R) F68 concentrations on the sol-gel transition temperature, which is an indicator of optimum formulations. The optimized formulation was a free-flowing liquid below 30.9 degrees C that transformed into a semi-solid gel above 34.2 degrees C after dilution with simulated tear fluid. Results of the in vitro release and erosion behavior study indicated that Cur-BSA-NPs-Gel achieved superior sustained-release effects and that incorporation of albumin nanoparticles exerted minimal effects on the gel structure. In addition, in vivo-ophthalmic experiments employing Cur-BSA-NPs-Gel were subsequently performed in rabbits. In vivo eye irritation results showed that Cur-BSA-NPs-Gel might be considered safe for ophthalmic drug delivery. The in vivo study also revealed that the formulation could significantly increase curcumin bioavailability in the aqueous humor. In conclusion, the optimized in situ gel-formulation developed in this work has significant potential for ocular application.
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