Studying the influence of formulation and process variables on Vancomycin-loaded polymeric nanoparticles as potential carrier for enhanced ophthalmic delivery
Yousry C.; Elkheshen S.A.; El-laithy H.M.; Essam T.; Fahmy R.H.
Date issued:
2017
Publisher:
Elsevier B.V.
Series Info:
European Journal of Pharmaceutical Sciences
100
Type:
Article
Keywords:
Draize test
,
Microbiological susceptibility testing
,
Ocular infection
,
Poly (D,L-lactide- coglycolide) (PLGA)
,
Polycaprolactone (PCL)
,
Vancomycin
,
carbomer
,
eudragit
,
nanoparticle
,
polymer
,
solvent
,
sorbitan oleate
,
vancomycin
,
acrylic acid resin
,
antiinfective agent
,
drug carrier
,
eudragit rs
,
gel
,
nanoparticle
,
vancomycin
,
animal tissue
,
area under the curve
,
Article
,
controlled study
,
drug bioavailability
,
drug delivery system
,
drug formulation
,
drug release
,
emulsion
,
encapsulation
,
factorial design
,
in vivo study
,
maximum plasma concentration
,
nonhuman
,
particle size
,
priority journal
,
ultrasound
,
zeta potential
,
animal
,
chemistry
,
drug effects
,
drug formulation
,
gel
,
intraocular drug administration
,
pH
,
rabbits and hares
,
Staphylococcus aureus
,
Acrylic Resins
,
Administration, Ophthalmic
,
Animals
,
Anti-Bacterial Agents
,
Drug Carriers
,
Drug Compounding
,
Drug Liberation
,
Gels
,
Hydrogen-Ion Concentration
,
Nanoparticles
,
Rabbits
,
Staphylococcus aureus
,
Vancomycin
Abstract:
Ocular topically applied Vancomycin (VCM) suffers poor bioavailability due to its high molecular weight and hydrophilicity. In the present investigation, VCM-loaded polymeric nanoparticles (PNPs) were developed aiming to enhance its ocular bioavailability through prolonging its release pattern and ophthalmic residence. PNPs were prepared utilizing double emulsion (W/O/O), solvent evaporation technique. 23 � 41 full factorial design was applied to evaluate individual and combined influences of polymer type, Eudragit� RS100, sonication time, and Span�80 concentration on PNPs particle size, encapsulation efficiency, and zeta potential. Further, the optimized formulae were incorporated in 1% Carbopol�-based gel. In-vivo evaluation of the optimized formulae was performed via Draize test followed by microbiological susceptibility testing on albino rabbits. Results revealed successful formulation of VCM-loaded PNPs was achieved with particle sizes reaching 155 nm and up to 88% encapsulation. Draize test confirmed the optimized formulae as non-irritating and safe for ophthalmic administration. Microbiological susceptibility testing confirmed prolonged residence, higher Cmax. with more than two folds increment in the AUC(0.25�24) of VCM-PNPs over control groups. Thus, VCM-loaded PNPs represent promising carriers with superior achievements for enhanced Vancomycin ophthalmic delivery over the traditional use of commercially available VCM parenteral powder after constitution into a solution by the ophthalmologists. � 2017 Elsevier B.V.
Show full item record