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[Chitosan-coated ophthalmic submicro emulsion for pilocarpine nitrate].
Yao Xue Xue Bao 2011; 46(8):990-6YX

Abstract

The study is to design chitosan-coated pilocarpine nitrate submicro emulsion (CS-PN/SE) for the development of a novel mucoadhesive submicro emulsion, aiming to prolong the precorneal retention time and improve the ocular absorption. CS-PN/SE was fabricated in two steps: firstly, pilocarpine nitrate submicro emulsion (PN/SE) was prepared by high-speed shear with medium chain triglycerides (MCT) as oil phase and Tween 80 as the main emulsifier, and then incubated with chitosan (CS) acetic solution. The preparation process was optimized by central composite design-response surface methodology. Besides the particle size, zeta potential, entrapment efficiency and micromorphology were investigated, CS-PN/SE's precorneal residence properties and miotic effect were especially studied using New Zealand rabbits as the animal model. When CS-PN/SE was administered topically to rabbit eyes, the ocular clearance and the mean resident time (MRT) of pilocarpine nitrate were found to be dramatically improved (P < 0.05) compared with PN/SE and pilocarpine nitrate solution (PNs), since the K(CS-PN/SE) was declined to 0.006 4 +/- 0.000 3 min(-1) while MRT was prolonged up to 155.4 min. Pharmacodynamics results showed that the maximum miosis of CS-PN/SE was as high as 46.3%, while the miotic response lasted 480 min which is 255 min and 105 min longer than that of PNs and PN/SE, respectively. A larger area under the miotic percentage vs time curve (AUC) of CS-PN/SE was exhibited which is 1.6 folds and 1.2 folds as much as that of PNs and PN/SE, respectively (P < 0.05). Therefore, CS-PN/SE could enhance the duration of action and ocular bioavailability by improving the precorneal residence and ocular absorption significantly.

Authors+Show Affiliations

Pharmaceutical Research Institute, China Pharmaceutical University, Nanjing 210009, China.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

English Abstract
Journal Article

Language

chi

PubMed ID

22007526

Citation

Wei, Jun, et al. "[Chitosan-coated Ophthalmic Submicro Emulsion for Pilocarpine Nitrate]." Yao Xue Xue Bao = Acta Pharmaceutica Sinica, vol. 46, no. 8, 2011, pp. 990-6.
Wei J, He HL, Zheng CL, et al. [Chitosan-coated ophthalmic submicro emulsion for pilocarpine nitrate]. Yao Xue Xue Bao. 2011;46(8):990-6.
Wei, J., He, H. L., Zheng, C. L., & Zhu, J. B. (2011). [Chitosan-coated ophthalmic submicro emulsion for pilocarpine nitrate]. Yao Xue Xue Bao = Acta Pharmaceutica Sinica, 46(8), pp. 990-6.
Wei J, et al. [Chitosan-coated Ophthalmic Submicro Emulsion for Pilocarpine Nitrate]. Yao Xue Xue Bao. 2011;46(8):990-6. PubMed PMID: 22007526.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - [Chitosan-coated ophthalmic submicro emulsion for pilocarpine nitrate]. AU - Wei,Jun, AU - He,Hong-Liang, AU - Zheng,Chun-Li, AU - Zhu,Jia-Bi, PY - 2011/10/20/entrez PY - 2011/10/20/pubmed PY - 2013/3/19/medline SP - 990 EP - 6 JF - Yao xue xue bao = Acta pharmaceutica Sinica JO - Yao Xue Xue Bao VL - 46 IS - 8 N2 - The study is to design chitosan-coated pilocarpine nitrate submicro emulsion (CS-PN/SE) for the development of a novel mucoadhesive submicro emulsion, aiming to prolong the precorneal retention time and improve the ocular absorption. CS-PN/SE was fabricated in two steps: firstly, pilocarpine nitrate submicro emulsion (PN/SE) was prepared by high-speed shear with medium chain triglycerides (MCT) as oil phase and Tween 80 as the main emulsifier, and then incubated with chitosan (CS) acetic solution. The preparation process was optimized by central composite design-response surface methodology. Besides the particle size, zeta potential, entrapment efficiency and micromorphology were investigated, CS-PN/SE's precorneal residence properties and miotic effect were especially studied using New Zealand rabbits as the animal model. When CS-PN/SE was administered topically to rabbit eyes, the ocular clearance and the mean resident time (MRT) of pilocarpine nitrate were found to be dramatically improved (P < 0.05) compared with PN/SE and pilocarpine nitrate solution (PNs), since the K(CS-PN/SE) was declined to 0.006 4 +/- 0.000 3 min(-1) while MRT was prolonged up to 155.4 min. Pharmacodynamics results showed that the maximum miosis of CS-PN/SE was as high as 46.3%, while the miotic response lasted 480 min which is 255 min and 105 min longer than that of PNs and PN/SE, respectively. A larger area under the miotic percentage vs time curve (AUC) of CS-PN/SE was exhibited which is 1.6 folds and 1.2 folds as much as that of PNs and PN/SE, respectively (P < 0.05). Therefore, CS-PN/SE could enhance the duration of action and ocular bioavailability by improving the precorneal residence and ocular absorption significantly. SN - 0513-4870 UR - https://www.unboundmedicine.com/medline/citation/22007526/[Chitosan_coated_ophthalmic_submicro_emulsion_for_pilocarpine_nitrate]_ DB - PRIME DP - Unbound Medicine ER -