Antibiotics delivered through conventional dosage against ophthalmic infections show lower therapeutic efficacy due to their low residence time. Therefore, there is a great need to design and develop novel dosage forms that would increase the ocular residence time of antibiotics at the site of infection. This study describes the development of nanoparticles laden in situ gelling solution, intended to sustain antibiotic release for improved therapeutic efficiency. Oxytetracycline-loaded gelatin-polyacrylic acid nanoparticles were prepared and incorporated in poloxamer-N407 solution. The rheological properties of the system were studied concerning time and temperature. Moreover, in vivo biocompatibility of the system was ascertained using the Draize test and histological studies. Finally, the optimized formulation was evaluated for in vitro antibacterial activity against one of the most common keratitis causing bacteria, Pseudomonas aeruginosa. Additionally, the in vivo efficacy was evaluated on the rabbit’s eye conjunctivitis model. The formulation showed a sustained effect against keratitis; furthermore, the antibacterial activity was comparable with the commercial product.
The aim of this study is to formulate polymeric paclitaxel nanoparticles with various stabilizers to improve solubility, enhance stability, maximize therapeutic efficacy and minimize detrimental toxicities of paclitaxel. In this study, trastuzumab-guided poly lactic-co-glycolic acid (PLGA)-loaded paclitaxel nanoparticles were formulated with pluronic F-127, polyvinyl alcohol (PVA), poloxamer 407, Tween-80, span 20, sodium dodecyl sulfate (SDS), and sodium lauryl sulfate (SLS) at different concentrations (0.5, 1, 1.5 and 2%) using the solvent evaporation method. The nanoparticles were evaluated for physicochemical characteristics and short and long-term stability. The optimum particle size (190 nm ± 12.42 to 350 nm ± 11.1), PDI (0.13 ± 0.02 to 0.2 ± 0.01), surface charge (-19.1mv ± 1.5 to −40.4mv ± 1.6), drug loading (2.43 to 9.5 %) and encapsulation efficiency (greater than 80 %) were obtained with these stabilizers while keeping the polymer concentration, temperature, probe size, amplitude and sonication time constant. The nanoformulations were stably stored at 4 °C. The nanoformulations of paclitaxel with pluronic F-127, polyvinyl alcohol (PVA), and poloxamer 407 were found to be more soluble, stable, uniform in physicochemical properties, and efficient in drug loading and encapsulation for improved therapeutic effects.
This study was to designed to develop sorafenib-loaded polymeric nanoparticles, surface-modified with pluronic F-127 for the effective treatment of hepatocellular (HCC) and renal cell carcinomas (RCC). Poly lactic coglycolic acid (PLGA) was used to encapsulate different concentrations of sorafenib by a simple modified solvent evaporation method applying pluronic F-127 as a surfactant and coating agent. The preformulation and characterization studies were conducted to evaluate the incompatibilities among sorafenib, PLGA and pluronic F-127, and physicochemical properties of the formulations, respectively. The sizes of the coated and plain PLGA nanoparticles were ~140 ± 14.7 nm and ~ 120 ± 10.1 nm, respectively. It has been confirmed from the in vitro release studies that PLGA sustained the release of sorafenib, avoiding the initial burst release, while the in vivo studies demonstared that surface-modified nanoparticles have greater affinity in the target aorgans than plain PLGA nanoparticles and free drug keeping the dose constant (20 mg/kg body weight). The delivery of sorafenib-loaded polymeric PLGA nanoparticles into the target tissues and their pharmacokinetic parameters have been improved significantly compared to the reported formulations.