Formulation and Characterization of Carvedilol Leciplex for Glaucoma Treatment: In-Vitro, Ex-Vivo and In-Vivo Study

Abstract

This study evaluated the efficacy of cationic nanoparticle (leciplex) to deliver carvedilol to ocular surface for glaucoma treatment as recent studies pointed out the effect of topical carvedilol on intraocular pressure, therefore carvedilol loaded leciplex formulae were prepared using soy phosphatidyl choline (SPC) and cationic surfactant (CTAB/DDAB) and characterized for morphology, entrapment efficiency, particle size, zeta potential and ex-vivo corneal permeation. Then the selected formula was evaluated via in-vivo studies in comparison with carvedilol solution. Leciplex nanoparticles appeared spherical in shape with entrapment efficiency exceeded 95% in all formulae. Leciplex formula composed of SPC and DDAB in (1:1) molar ratio showed the smallest particle size (16.04 ± 1.2 nm), highest zeta potential value (53.9 ± 0.91 mv) and highest apparent corneal permeability coefficient (0.1157 cm/h). Carvedilol leciplex reduced intraocular pressure (IOP) to normal range in ocular hypertensive rabbits after 30 min and duration of action lasted for 24 h, while carvedilol solution reduced IOP to normal value after 60 min and duration of action lasted for 6 h. Furthermore, histological examination of eyeballs of rabbits treated with carvedilol leciplex showed improvement of retinal atrophy of glaucomatous eyes. This study concluded that leciplex improve transcorneal permeation and bioavailability of carvedilol.

Spironolactone-Loaded LeciPlexes as Potential Topical Delivery Systems for Female Acne: In Vitro Appraisal and Ex Vivo Skin Permeability Studies

“…This indicates that maximum drug encapsulation was achieved at SP amount of 30 mg, after which excess drug was precipitated, leading to decreased encapsulation efficiency. Other drug-loaded LeciPlex systems showed drug encapsulation efficiency of ≥90% [30,31,42]. The increase in drug encapsulation was accompanied with an increase in particle size from 337 ± 11.06 to 591 ± 13.7 nm, after which the size decreased with further increase in drug concentration.…”

“…SP-loaded LeciPlexes were prepared as outlined above using various drug amounts (10,20,30,40, and 50 mg) at CTAB/PL-90G molar ratio of 1:1, and their properties were evaluated.…”

“…LeciPlex preparations were shown to enhance the bioavailability of various drugs. For instance, LeciPlexes improved the ocular bioavailability and transcorneal permeability of carvedilol [30]. They also improved the anti-inflammatory and antitumor activity of quercetin compared to drug suspension upon oral administration [31].…”

<p>Nanogel loaded with surfactant based nanovesicles for enhanced ocular delivery of acetazolamide</p>

“…Each measurement was repeated for three readings. IOP was measured with a tonometer (Riester, Germany) under surface anesthesia using 0.2% lidocaine 25…”

Promising Approach in the Treatment of Glaucoma Using Nanotechnology and Nanomedicine-Based Systems

“…Hassan et al [68] in new research, studied the use of cationic nanoparticle (leciplex) in carvedilol delivery to ocular surfaces as a glaucoma therapy since other research [69,70] illustrated that carvedilol had an effect on intraocular pressure. As such, the leciplex formulae filled with carvedilol were made with cationic surfactant (CTAB/DDAB), soy phosphatidylcholine (SPC), and characterizations were done.…”