Please use this identifier to cite or link to this item: https://doi.org/10.1371/journal.pone.0024513
Title: Sustained release of an Anti-Glaucoma drug: Demonstration of efficacy of a liposomal formulation in the rabbit eye
Authors: Natarajan J.V.
Chattopadhyay S.
Ang M. 
Darwitan A.
Foo S.
Zhen M.
Koo M.
Wong T.T. 
Venkatraman S.S.
Keywords: antiglaucoma agent
dipalmitoylphosphatidylcholine
drug carrier
latanoprost
liposome
antihypertensive agent
latanoprost
liposome
prostaglandin F
animal experiment
animal tissue
article
concentration (parameters)
controlled study
differential scanning calorimetry
drug delivery system
drug dosage form comparison
drug efficacy
drug storage
female
in vitro study
lipid bilayer
molecular stability
nonhuman
rabbit
sustained release formulation
animal
chemistry
conjunctiva
delayed release formulation
drug effect
glaucoma
methodology
topical drug administration
Oryctolagus cuniculus
1,2-Dipalmitoylphosphatidylcholine
Administration, Topical
Animals
Antihypertensive Agents
Calorimetry, Differential Scanning
Conjunctiva
Delayed-Action Preparations
Drug Carriers
Drug Delivery Systems
Female
Glaucoma
Lipid Bilayers
Liposomes
Prostaglandins F, Synthetic
Rabbits
Issue Date: 2011
Citation: Natarajan J.V., Chattopadhyay S., Ang M., Darwitan A., Foo S., Zhen M., Koo M., Wong T.T., Venkatraman S.S. (2011). Sustained release of an Anti-Glaucoma drug: Demonstration of efficacy of a liposomal formulation in the rabbit eye. PLoS ONE 6 (9) : e24513. ScholarBank@NUS Repository. https://doi.org/10.1371/journal.pone.0024513
Abstract: Topical medication remains the first line treatment of glaucoma; however, sustained ocular drug delivery via topical administration is difficult to achieve. Most drugs have poor penetration due to the multiple physiological barriers of the eye and are rapidly cleared if applied topically. Currently, daily topical administration for lowering the intra-ocular pressure (IOP), has many limitations, such as poor patient compliance and ocular allergy from repeated drug administration. Poor compliance leads to suboptimal control of IOP and disease progression with eventual blindness. The delivery of drugs in a sustained manner could provide the patient with a more attractive alternative by providing optimal therapeutic dosing, with minimal local toxicity and inconvenience. To investigate this, we incorporated latanoprost into LUVs (large unilamellar vesicles) derived from the liposome of DPPC (di-palmitoyl-phosphatidyl-choline) by the film hydration technique. Relatively high amounts of drug could be incorporated into this vesicle, and the drug resides predominantly in the bilayer. Vesicle stability monitored by size measurement and DSC (differential scanning calorimetry) analysis showed that formulations with a drug/lipid mole ratio of about 10% have good physical stability during storage and release. This formulation demonstrated sustained release of latanoprost in vitro, and then tested for efficacy in 23 rabbits. Subconjunctival injection and topical eye drop administration of the latanoprost/liposomal formulation were compared with conventional daily administration of latanoprost eye drops. The IOP lowering effect with a single subconjunctival injection was shown to be sustained for up to 50 days, and the extent of IOP lowering was comparable to daily eye drop administration. Toxicity and localized inflammation were not observed in any treatment groups. We believe that this is the first demonstration, in vivo, of sustained delivery to the anterior segment of the eye that is safe and efficacious for 50 days. © 2011 Natarajan et al.
Source Title: PLoS ONE
URI: https://scholarbank.nus.edu.sg/handle/10635/162033
ISSN: 19326203
DOI: 10.1371/journal.pone.0024513
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