Latanoprost loaded Phytantriol Cubosomes for Glaucoma Treatment

BESSONE CAROLINA; AKHLAGHI, S. P.; DANIELA QUINTEROS; LOH WATSON; DANIEL ALLEMANDI

Mar del Plata

Congreso; S A I C . S A F E . S A B . SAP 2 0 1 9 Participan AACYTAL . NANOMED-AR . HCS; 2019

Nanomed

Glaucoma is a degenerative optic neuropathy, itis characterized by increased intraocular pressure (IOP) that results in irreversible damages in all ocular nervous structures and is the main risk factor that can be modified and treated.Liquid crystal systems, such as cubosomes (CUB), emerge as a new way of transporting drugs with properties as biodegradables, bioadhesives and besides show a prolonged release, which makes as potentially useful for administration ocular. Latanoprost (LN) is an esterified prodrug that has a lipophilic nature, it reduces IOP through drainage of the aqueous humor.The principal goal was obtaining nanometric sized CUB through Top-down (TD) method and encapsulating LN for the treatment of glaucoma. TDapproach was employed to prepare CUBof phytantriol in water with a solution of Pluronic®F127 as a stabilizer using ultrasonication. CUB were prepared at different concentrations of LN. The average particle size and zeta potential were measured using DLS. The CUB was characterized using small-angle X-ray scattering (SAXS) and Isothermal titration calorimetry. The loading capacity was determined by HPLC. The in vitro release of LN from the CUB was studied using a dialysis method in cells coupled with LC/MS technique. To evaluate in vivo efficiency, the formulations were administered subconjuntival manner in normotensive rabbits. IOPand irritation were evaluated.The CUB had an average particle size of 200 nm with negative zeta potential values and it showed a good encapsulation efficiency of LNaround 90%. The SAXS studies revealed a double diamond Pn3m cubic structure for blank and LN-loaded CUB with an constant in the lattice parameter. The ITC assays showing an slight exothermic process of interaction between CUB and the drug. In vitro release essays exhibited a sustained release in the time at each concentration evaluated. Finally, in vivo essays showed animportant reduction of the IOP for 4 days without signal of significant irritation.