Effect of Ion Pairing on In Vitro Transcorneal Permeability of a Δ9-Tetrahydrocannabinol Prodrug: Potential in Glaucoma Therapy

In glaucoma therapy, nanoparticles (NPs) are a favorable tool for delivering drugs to the outflow tissues of the anterior chamber of the eye where disease development and progression take place. In this context, a prerequisite is an efficient enrichment of NPs in the trabecular meshwork with minimal accumulation in off-target tissues such as the cornea, lens, iris and ciliary body. We evaluated the optimal size for targeting the trabecular meshwork by using gold NPs of 5, 60, 80 and 120 nm with a bare surface (AuNPs) or coated with hyaluronic acid (HA-AuNPs). NPs were compared regarding their colloidal stability, distribution in the anterior chamber of the eye ex vivo and cellular uptake in vitro. HA-AuNPs demonstrated an exceptional colloidal stability. Even after application into porcine eyes ex vivo, the HA coating prevented an aggregation of NPs inside the trabecular meshwork. NPs with a diameter of 120 nm exhibited the highest volume-based accumulation in the trabecular meshwork. Off-target tissues in the anterior chamber demonstrated an exceptionally low gold content. Our findings are particularly important for NPs with encapsulated anti-glaucoma drugs because a higher particle volume would be accompanied by a higher drug payload.

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Enhancement and in vitro evaluation of amifostine permeation through artificial membrane (PAMPA) via ion pairing approach and mechanistic selection of its optimal counter ion

European Journal of Pharmaceutical Sciences ◽

10.1016/j.ejps.2013.10.002 ◽

2014 ◽

Vol 51 ◽

pp. 218-223 ◽

Cited By ~ 12

Author(s):

N. Samiei ◽

A. Shafaati ◽

A. Zarghi ◽

H.R. Moghimi ◽

S.M. Foroutan

Keyword(s):

Ion Pairing ◽

Artificial Membrane ◽

In Vitro Evaluation ◽

Counter Ion ◽

Selection Of

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OFLOXACIN ION PAIRING WITHIN SUBMICRON EMULSION: A POTENTIAL APPROACH FOR OCULAR DELIVERY

INDIAN DRUGS ◽

10.53879/id.56.04.11490 ◽

2019 ◽

Vol 56 (04) ◽

pp. 37-44

Author(s):

D Pandey ◽

R Singh ◽

S Jain ◽

D Jain ◽

Keyword(s):

Antimicrobial Activity ◽

Partition Coefficient ◽

Ion Pairing ◽

Sodium Deoxycholate ◽

Free Drug ◽

Ocular Delivery ◽

Potential Approach ◽

Ocular Infections ◽

Submicron Emulsion

The aim of the work was to improve the entrapment of ofloxacin within the submicron emulsion by ion pairing with sodium deoxycholate to improve antimicrobial activity and precorneal retention. Partition coefficient of ofloxacin-sodium deoxycholate was found to be 3.788, compared to 0.113 for the drug alone. Formulation was characterized for globules size 0.143 ± 0.07 μm, viscosity 3.8 ± 0.2 cP and pH, 7.1 ± 0.3. The entrapment was 80 ± 1% for ofloxacin-sodium deoxycholate in submicron emulsion compared to 57 ± 2% for the drug alone. More than 90% drug remained after 90 days in optimized formulations and was found stable. SEM confirmed droplets size to be 200 nm and spherical. Drug released 53.16% after 24 h from optimized formulation. In vitro antimicrobial efficacy improved against S. aureus as compared to free drug. No toxicity of optimized formulation on HET-CAM test was observed. Designed formulation may hold some promise for severe ocular infections where frequent dosing is required.

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