Page 34 - 2019

Ph.D.
(Parmacy)
DEVELOPMENT, OPTIMIZATION AND CHARACTERIZATION OF BESIFLOXACIN
HYDROCHLORIDE NANOFORMULATIONS FOR OCULAR DRUG DELIVERY

Ph.D. Scholar : Bijit Saha
Research Supervisor : Dr. Rakesh P. Patel

Regi. No.: 14146021002
Abstract :
The aim of present research is to design and development of solid lipid nanoparticle,
nanosuspension, nanoemulsion and niosome as an in-situ gel for ocular drug delivery of
Besifloxacin hydrochloride, a fourth generation fluoroquinolone antibiotic. Analytical
method of Besifloxacin Hydrochloride was developed by HPLC-UV technique. Various
characterization studies like FTIR, DSC, XRD were performed to check the compatibility
study with drug and excipients. SLN is prepared by Hot Homogenization Process using
glyceryl monostearate and polysorbate 80 along with poloxamer 188 and purified water.
Nanosuspension of Besifloxacin HCl was prepared by high speed homogenization
process using eudragit RS100, ethyl acetate, polysorbate 80, poloxamer 188 and purified
water. Nanoemulsion of Besifloxacin HCl was prepared by high speed homogenization
process using egg lechithin, soybean oil, glycerin, polysorbate 80, poloxamer 188 and
purified water. Niosome of Besifloxacin HCl was prepared by coacervation phase
separation method using cholesterol, span 60, ethanol and purified water. The preliminary
formulation of solid lipid nanoparticle, nanosuspension, nanoemulsion and niosome were
tested for zeta potential, polydispersity index, and particle size. The formulations were
optimized following 32 factorial design. Particle size, polydispersity index, zeta potential
and entrapment efficiency were evaluated for the confirmation of nanoformulations. The
final optimized formulations of solid lipid nanoparticle, nanosuspension, nanoemulsion
and niosome were mixed with optimized gelrite solution to form in-situ gel. Surface
morphology of final ophthalmic formulations were confirmed with SEM and TEM studies.
In-vitro releases were studies of above nanoformulations. Stability studies of final
ophthalmic nanoformulations were checked for 6 months as per the ICH guidelines.
Finally In-vivo studies of these solid lipid nanoparticles, nanosuspension, nanoemulsion
and niosome ophthalmic formulations were carried out with eye irritancy test and
compared with marketed formulations. From the development, optimization and
characterization of Besifloxacin hydrochloride loaded nanoformulations, it is concluded
that solid lipid nanoparticles, nanosuspension, nanoemulsion and niosome formulations
were showed the satisfactory outcomes for long acting ocular nanoformulation and
suggested for scale up in future. Among all the developed ophthalmic nanoformulations
solid lipid nanoparticles of Besifloxacin Hydrochloride found better release profile for

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