Spanlastics nanovesicular ocular insert as a novel ocular delivery of travoprost: optimization using Box-Behnken design and in vivo evaluation.

Currently, travoprost is a synthetic prostaglandin F2α analogue used in the treatment of glaucoma, it is delivered by eye drop solution. Due to its very low bioavailability and patient non-compliance, the objective of the current study was to enhance its bioavailability, and prolong its release Spanlastic nano-vesicles gels were designed and optimized using Box-Behnken design. The optimized spanlastic nano-vesicles gel exhibited the lowest particle size (PS), polydispersity index (PDI) and the highest zeta potential (ZP), encapsulation efficiency (EE) and mucoadhesive strength was fabricated into spanlastic nano-vesicles ocular insert by solvent casting. In vivo studies showed enhanced bioavailability of travoprost spanlastic nano-vesicles gel and ocular insert compared to the marketed eye drops (travoswix®), as proven by their higher Cmax and AUC0-∞, in addition to being nonirritant to ocular surfaces. However, spanlastic nano-vesicles ocular insert showed more prolonged effect than spanlastic nano-vesicles gel. According to our study, it can be suggested that travoprost spanlastic nano-vesicles ocular insert is a novel ocular delivery system for glaucoma treatment.

Enhancement of the ocular therapeutic effect of prednisolone acetate by liposomal entrapment.

Eye drops account for 90% of ophthalmic formulations despite of the rapid precorneal drug loss. Our aim is to test the effect of positive charge induction and the subsequent size reduction on the efficiency of liposomes as ocular drug delivery system for the lipophilic drug prednisolone acetate (PSA). Different formulations of PSA-loaded liposomes, positive multilamellar liposomes (pMLV), positive small (nano-sized) unilamellar liposomes (pSUV) and neutral multilamellar liposomes (nMLV), were prepared. These formulations were characterized by measuring surface charge, size distribution, entrapment efficiency, release rate, and ability to deliver PSA across the cornea. In vitro studies showed that positive charge induction reduces the transcorneal flux (about 1.9-fold lower than nMLV), while the subsequent size reduction results in higher flux (about 1.2-fold higher than nMLV). But in vivo results revealed that pSUV produced more concentrations of PSA in aqueous humor than nMLV (P < 0.05) suggesting greater chance for drug penetration, pSUV were more effective than nMLV in this regard (P < 0.05). As revealed by in vivo studies and ophthalmic examinations, positive charge induction and the subsequent size reduction increased the efficiency of liposomes as ocular drug delivery system for PSA.

Efficacy of topically applied liposome-bound tetracycline in the treatment of dry eye model.

OBJECTIVE: To evaluate the effects of liposome-bound tetracycline eye drops in a rabbit dry eye model evaluating their advantage of being less allergic, preservative free and prolonged action compared with other tear substitutes. PROCEDURES: New Zealand albino rabbits were equally divided into control group and dry eye induced groups. Dryness was induced in 24 eyes of 12 healthy adult male albino rabbits by instilling atropine sulfate eye drops 1% three times daily for 1 week, then animals were subdivided into four groups; group 1 (rabbits with dry eye model), groups 2, 3, and 4: rabbits with dry eye model treated for 7 days starting on 7th day of dryness induction with either tetracycline, empty liposome, or combined tetracycline with liposome as topical eye drops respectively. Schirmer (STT) test and tear break up time (TBUT) were assessed on days 0, 2, 4, 7, 9, 11, and 14. Animals were sacrificed on day 14 and histopathological examination of the cornea and conjunctiva was performed. RESULTS: Tear break up time and STT test values were significantly improved in groups 2, 3, 4 as compared with group 1. The histopathological examination showed normal cytoarchitecture of corneas and conjunctivae in groups 2, 3, 4 against the dryness effect that continued to affect the cornea and conjunctival epithelium in group 1. There was a significant improvement in the group treated with liposome-bound tetracycline eye drops (group 4) as compared with tetracycline alone (group 2) and empty liposome (group 3). CONCLUSION: The use of liposome encapsulated tetracycline significantly improved STT and TBUT values as well as reverse surface ocular pathology.