Author(s)

Dongzhi Hou^1*, Ruyi Gui¹, Sheng Hu¹, Yi Huang¹, Zuyong Feng², Qineng Ping³

¹College of Pharmacy, Guangdong Pharmaceutical University, Guangzhou, China.
²School of Physics and Optoelectronic Engineering, Guangdong University of Technology, Guangzhou, China.
³College of Pharmacy, China Pharmaceutical University, Nanjing, China.

The objective of the study was to investigate the potential of montmorillonite as a sustained carrier in the preparation of drug-loaded nanoparticles for prolonged ocular application. Nanoparticles were prepared by ionic gelation of chitosan with sodium tripolyphosphate (TPP). Betaxolol hydrochloride (BH) was applied as a model drug. TG, FT-IR, TEM, DLS and XRD have been employed in the characterization of drug-encapsulated chitosan-montmorillonite/TPP nanoparticles (CS-MMT/TPP NPs). TEM images showed that the particles were spherical in shape and had a rough surface. The size range of the nanoparticles was between 338 and 585 nm with positive zeta potential values from 24 mV to 36 mV and encapsulation efficiency values ranging from 12.27% to 50.92%. In vitro sustained drug release was observed with the BH-loaded nanoparticles in artificial tears (pH 7.4). The results of FT-IR, TG and XRD showed that the drug was coated with CSMMT/ TPP NPs. In the mucoadhesion studies, an interaction was found between drug-loaded CSMMT/ TPP NPs and mucin, which could enhance precorneal residence time and hence facilitate an effective sustained release. The optimized formulation was determined to be non-irritant and tolerable by modified Draize test. Therefore, the BH-loading CS-MMT/TPP NPs developed are a promising carrier for controlled drug delivery to the eye.

Chitosan, Montmorillonite, Nanoparticles, Mucoadhesive, Sustained Release, Ocular Irritation

Hou, D. , Gui, R. , Hu, S. , Huang, Y. , Feng, Z. and Ping, Q. (2015) Preparation and Characterization of Novel Drug-Inserted-Montmorillonite Chitosan Carriers for Ocular Drug Delivery. Advances in Nanoparticles, 4, 70-84. doi: 10.4236/anp.2015.43009.