Novel mucoadhesive polysaccharide isolated from Bletilla striata improves the intraocular penetration and efficacy of levofloxacin in the topical treatment of experimental bacterial keratitis.

Abstract

OBJECTIVES:

The objective of the present study was to evaluate a novel mucoadhesive polymer extracted from Bletilla striata for ocular delivery of 0.5% levofloxacin in rabbits, and to determine its improved efficacy against experimental keratitis.

METHODS:

B. striata polysaccharide (BsP) was subjected to cell cytotoxicity and ferning tests. The pharmacokinetics and bioavailability of topically applied 0.5% levofloxacin-BsP eye drops was investigated and compared with 0.5% levofloxacin eye drops (Cravit). Experimental Staphylococcus aureus keratitis was induced and treated with levofloxacin or levofloxacin-BsP eye drops.

KEY FINDINGS:

BsP markedly increased the proliferative capacity of a human corneal epithelial [corrected] cell line. The ferning test showed that BsP exhibited optimal performance as a tear fluid. The polysaccharides significantly increased intra-aqueous penetration and corneal accumulation in rabbits. Treatment with levofloxacin-BsP reduced the number of organisms more significantly than eye drops containing levofloxacin alone.

CONCLUSIONS:

BsP appears to be a promising candidate as a vehicle for topical ophthalmic drug delivery, especially for antibiotics.

• Authors: Xiang-gen Wu, Meng Xin, Hao Chen, Li-na Yang, Hao-ran Jiang
• Journal: The Journal of pharmacy and pharmacology (J Pharm Pharmacol) Vol. 62 Issue 9 Pg. 1152-7 (Sep 2010) ISSN: 2042-7158 [Electronic] England
• PMID: 20796194 (Publication Type: Journal Article)

Chemical References

• Anti-Bacterial Agents
• Ophthalmic Solutions
• Plant Extracts
• Polysaccharides
• Levofloxacin
• Ofloxacin

Topics

• Absorption
• Administration, Topical
• Animals
• Anti-Bacterial Agents (pharmacokinetics, pharmacology, therapeutic use)
• Aqueous Humor (drug effects)
• Bacterial Load
• Biological Availability
• Cell Line
• Cell Proliferation (drug effects)
• Cornea (cytology, drug effects)
• Disease Models, Animal
• Endothelial Cells (drug effects, physiology)
• Eye (cytology, drug effects)
• Female
• Humans
• Keratitis (drug therapy, microbiology)
• Levofloxacin
• Male
• Ofloxacin (pharmacokinetics, pharmacology, therapeutic use)
• Ophthalmic Solutions
• Orchidaceae (chemistry)
• Plant Extracts (pharmacology)
• Polysaccharides (isolation & purification, pharmacology)
• Rabbits
• Staphylococcal Infections (drug therapy)
• Staphylococcus aureus (drug effects)
• Tears
• Treatment Outcome