Formulation and evaluation of micro hydrogel of Moxifloxacin hydrochloride

Abstract

The field of ocular drug delivery is one of the interesting and challenging endeavors facing the pharmaceutical scientist. Novel approaches for ophthalmic drug delivery need to be established to increase the ocular bioavailability by overcoming the inherent drawbacks of conventional dosage forms. In situ hydrogels are instilled as drops into the eye and undergoes a sol-to-gel transition in the cul-de-sac, improved ocular bioavailability by increasing the duration of contact with corneal tissue, thereby reducing the frequency of administration. The purpose of the present work was to develop an ophthalmic drug delivery system using three different gelling agents with different mechanisms for in situ gelation of Moxifloxacin hydrochloride, a fluoroquinolone antibiotic. polyox (a pH-sensitive gelling agent), sodium alginate (an ion-sensitive gelling agent), and poloxamer (a temperature-sensitive gelling agent) were employed for the formation of in situ hydrogel along with HPMC K4M as viscofying agent, which increases the residence time of the drug in the ocular cavity. The promising formulations MF(4), MF(5), and MF(9) were evaluated for pH, drug content, in vitro gelation, in vitro drug release, in vivo drug release, ocular irritation, and stability. Percent drug content of 98.2, 98.76, and 99.43%; viscosity of 15.724 × 100, 16.108 × 100, and 15.213 × 100 cP at 20 rpm, cumulative percent release of 75.364, 74.081, and 71.752%, and C (max) of 1,164.16, 1,187.09, and 1,220.58 ng/ml was observed for formulation MF(4), MF(5), and MF(9), respectively. The developed formulations were therapeutically efficacious, stable, and non-irritant and provided sustained release of the drug over 8 h.

Topical delivery of ocular therapeutics: carrier systems and physical methods

“…Considering the topical administration of hydrogels to the eye, researchers have claimed that hydrogels are more resistant to removal from the eye through blinking because of their viscoelastic properties. As a result, the formulation contact time with the ocular surface is increased in comparison to simple eye drops . Therefore, the requirement for repeated applications is reduced, and patient compliance is increased.…”

“…Currently, different polymers are blended to improve the gel characteristics for topical ocular delivery systems . Poloxamers, for example, have been widely studied as thermosensitive in‐situ‐forming gels, but they suffer the major drawback of having weak mechanical strength .…”

“…As a result, the formulation contact time with the ocular surface is increased in comparison to simple eye drops. [177,178] Therefore, the requirement for repeated applications is reduced, and patient compliance is increased.…”

“…[54,55,83,180] Currently, different polymers are blended to improve the gel characteristics for topical ocular delivery systems. [78,82,178] Poloxamers, for example, have been widely studied as thermosensitive in-situ-forming gels, [84,86,181] but they suffer the major drawback of having weak mechanical strength. [182] To solve this problem, poloxamers have been blended with polyacrylic acid, [183] alginate [85] and chitosan.…”

“…The in situ-forming gels are the most studied hydrogels because drug formulation is administered in eye drops, which enables a better control of the drug dosage. [98,[177][178][179] Contact lenses Prolonged drug delivery compared with eye drops. The incorporation of nanoparticles in the lens has been shown to prolong drug delivery and improve drug loading.…”