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Phase transition water-in-oil microemulsions as ocular drug delivery systems: in vitro and in vivo evaluation.
Int J Pharm. 2007 Jan 02; 328(1):65-71.IJ

Abstract

Microemuslion (ME)-based phase transition systems were evaluated for ocular delivery of pilocarpine hydrochloride (model hydrophilic drug). These used two non-ionic surfactants, sorbitan mono laurate and polyoxyethylene sorbitan mono-oleate with ethyl oleate (oil component) and water. These systems undergo phase change from ME to liquid crystalline (LC) and to coarse emulsion (EM) with a change in viscosity depending on water content. This study selected five formulations containing aqueous phase at 5% (w/w) (ME 5%), 10% (w/w) (ME 10%), 26% (w/w) (LC), 85% (w/w) (O/W EM) and 100% (solution) with the model drug at 1% (w/w). Incorporation of pilocarpine hydrochloride did not affect the phase behaviour. The viscosity was increased initially with dilution from ME 5% to ME 10% then LC, indicating structuring of the system, before being reduced in the EM formulation. Drug release depended on the viscosity with lower release rates obtained from formulations with high viscosity. The miotic response and duration of action were greatest in case of ME and LC formulations indicating high ocular bioavailability. Thus, phase transition ME is promising for ocular drug delivery as it provides the fluidity with its viscosity being increased after application increasing ocular retention while retaining the therapeutic efficiency.

Authors+Show Affiliations

School of Pharmacy, The University of Auckland, Auckland, New Zealand.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

17092668

Citation

Chan, Judy, et al. "Phase Transition Water-in-oil Microemulsions as Ocular Drug Delivery Systems: in Vitro and in Vivo Evaluation." International Journal of Pharmaceutics, vol. 328, no. 1, 2007, pp. 65-71.
Chan J, Maghraby GM, Craig JP, et al. Phase transition water-in-oil microemulsions as ocular drug delivery systems: in vitro and in vivo evaluation. Int J Pharm. 2007;328(1):65-71.
Chan, J., Maghraby, G. M., Craig, J. P., & Alany, R. G. (2007). Phase transition water-in-oil microemulsions as ocular drug delivery systems: in vitro and in vivo evaluation. International Journal of Pharmaceutics, 328(1), 65-71.
Chan J, et al. Phase Transition Water-in-oil Microemulsions as Ocular Drug Delivery Systems: in Vitro and in Vivo Evaluation. Int J Pharm. 2007 Jan 2;328(1):65-71. PubMed PMID: 17092668.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Phase transition water-in-oil microemulsions as ocular drug delivery systems: in vitro and in vivo evaluation. AU - Chan,Judy, AU - Maghraby,Gamal M M El, AU - Craig,Jennifer P, AU - Alany,Raid G, Y1 - 2006/10/07/ PY - 2005/11/15/received PY - 2006/08/28/revised PY - 2006/10/01/accepted PY - 2006/11/10/pubmed PY - 2007/2/27/medline PY - 2006/11/10/entrez SP - 65 EP - 71 JF - International journal of pharmaceutics JO - Int J Pharm VL - 328 IS - 1 N2 - Microemuslion (ME)-based phase transition systems were evaluated for ocular delivery of pilocarpine hydrochloride (model hydrophilic drug). These used two non-ionic surfactants, sorbitan mono laurate and polyoxyethylene sorbitan mono-oleate with ethyl oleate (oil component) and water. These systems undergo phase change from ME to liquid crystalline (LC) and to coarse emulsion (EM) with a change in viscosity depending on water content. This study selected five formulations containing aqueous phase at 5% (w/w) (ME 5%), 10% (w/w) (ME 10%), 26% (w/w) (LC), 85% (w/w) (O/W EM) and 100% (solution) with the model drug at 1% (w/w). Incorporation of pilocarpine hydrochloride did not affect the phase behaviour. The viscosity was increased initially with dilution from ME 5% to ME 10% then LC, indicating structuring of the system, before being reduced in the EM formulation. Drug release depended on the viscosity with lower release rates obtained from formulations with high viscosity. The miotic response and duration of action were greatest in case of ME and LC formulations indicating high ocular bioavailability. Thus, phase transition ME is promising for ocular drug delivery as it provides the fluidity with its viscosity being increased after application increasing ocular retention while retaining the therapeutic efficiency. SN - 0378-5173 UR - https://www.unboundmedicine.com/medline/citation/17092668/Phase_transition_water_in_oil_microemulsions_as_ocular_drug_delivery_systems:_in_vitro_and_in_vivo_evaluation_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(06)00811-8 DB - PRIME DP - Unbound Medicine ER -