<p>Clarithromycin-Loaded Ocular Chitosan Nanoparticle: Formulation, Optimization, Characterization, Ocular Irritation, and Antimicrobial Activity</p>

Abstract

The topically administered drugs through conventional delivery systems have low bioavailability. Henceforth, the present study was designed to prepare and optimize clarithromycin (CTM)-loaded chitosan nanoparticles (CHNPs) to demonstrate the efficacy against microorganisms. Methods: Clarithromycin-loaded chitosan nanoparticles (CTM-CHNPs) were prepared by ionotropic gelation method. The formulation was optimized by box-Behnken design using the formulation variables like CH (A), STPP concentration (B), and stirring speed (C). Their effects were evaluated on the independent variables like particle size (Y 1) and entrapment efficiency (Y 2). Further, CTM-CHNPs were evaluated for physicochemical parameters, invitro drug release, ex-vivo permeation, bioadhesive study, corneal hydration, histopathology, HET-CAM, and antibacterial study. Results: The optimized formulation (CTM-CHNPopt) showed the low particle size (152±5 nm), which is desirable for ocular delivery. It also showed high encapsulation (70.05%), zeta potential (+35.2 mV), and was found in a spherical shape. The drug release study revealed a sustained drug release profile (82.98±3.5% in 12 hours) with Korsmeyer peppas kinetic (R 2 =0.996) release model. It showed a 2.7-fold higher corneal permeation than CTMsolution. CHNPs did not exhibit any sign of damage to excised goat cornea, which is confirmed by hydration, histopathology, and HET-CAM test. It exhibited significant (P<0.05) higher antibacterial susceptibility than CTM-solution. Conclusion: The finding of the study concluded that CTM-CHNPs can be used for effective management of bacterial conjunctivitis by increasing the precorneal residence time.

Design and Optimization of New Enteric Nanoparticles of Ceftriaxone for Oral Delivery: In vitro and in vivo Assessments

“…Nanoparticles (NPs) made from natural biodegradable polymers are known for their small size, biodegradability, nontoxicity, and long shelf-life. [9][10][11] These merits make them a point of interest for targeted drug delivery. An interesting mean to attain NPs is through ionic gelation.…”

Effective Ocular Delivery of Eplerenone Using Nanoengineered Lipid Carriers in Rabbit Model

“…[10][11][12] Topical formulations to treat intraocular diseases face obstacles, limiting their delivery, including precorneal loss factors (eg, tear dynamics, transient residence time in the cul-de-sac, and relative impermeability of the corneal epithelial membrane), resulting in poor bioavailability. 13 In addition, the residence time of the drug on the corneal surface and drug penetration across the cornea still needs to be increased. 14 Modifying viscosity has been adopted to prolong corneal residence time by applying hydrogels or in situ gelling systems.…”

Combinatorial therapeutic drug delivery of riboflavin and dexamethasone for the treatment of keratoconus affected corneas of mice: Ex vivo permeation and hemolytic toxicity

“…Fortunately, there occurs no total blindness in this disease. Clinical symptoms also differ depending upon the severity of disease which includes external signs as Munson's sign (a characteristic feature of keratoconus in which there is protrusion of V-shape for the lower eyelid) and Rizzuti Phenomenon (which occurs in the nose area containing the bright reflection when light is exposed from nasal area) [6][7][8].…”

“…Keratoconus appears spontaneously and only few cases are from genetic transmission. The disease generally occurs at puberty stage and lasts for three to four decades or may occur at any stage of life [8]. Depending on the morphology classification, keratoconus is classified as: nipple -the diameter of cone is less than 5 mm which is observed in central or paracentral of the cornea, oval -the cone diameter is more than 5 mm which is observed in paracentral location, keratoglobus -the cone is observed in 75% of the cornea.…”

“…Some natural polymers and synthetic polymers can be used to sustain the action of the drug. Colloidal also has better acceptance in ocular drug delivery as it lessens the dose administration and avoids eye irritation [8]. The problems which are associated in the occular drug delivery can be overcome by formulating the thermoreversible gel or in situ gel.…”