The nonnucleoside reverse transcriptase inhibitors, used for the treatment of HIV infections, are reported to have low bioavailability pertaining to high first-pass metabolism, high protein binding, and enzymatic metabolism. They also show low permeability across blood brain barrier. The CNS is reported to be the most important HIV reservoir site. In the present study, solid lipid nanoparticles of efavirenz were prepared with the objective of providing increased permeability and protection of drug due to biocompatible lipidic content and nanoscale size and thus developing formulation having potential for enhanced bioavailability and brain targeting. Solid lipid nanoparticles were prepared by high pressure homogenization technique using a systematic approach of design of experiments (DoE) and evaluated for particle size, polydispersity index, zeta potential, and entrapment efficiency. Particles of average size 108.5 nm having PDI of 0.172 with 64.9% entrapment efficiency were produced. Zeta potential was found to be −21.2 mV and the formulation was found stable. The in-vivo pharmacokinetic studies revealed increased concentration of the drug in brain, as desired, when administered through intranasal route indicating its potential for an attempt towards complete eradication of HIV and cure of HIV-infected patients.

The development of a meaningful dissolution procedure for drug products with limited water solubility has been a challenge to the pharmaceutical industry. Aceclofenac (BCS Class II drug) is a nonsteroidal anti-inflammatory drug. There is no official dissolution medium available in the literature. In the present study, parameters such as solubility, medium pH, surfactant type, dissolution behavior of formulations, influence of sink conditions, stability, and discriminatory effect of dissolution testing were studied for the selection of a proper dissolution medium. Results of solubility data revealed that solubility increased with an increase in pH. Sink conditions were exhibited in all media except double-distilled water and 0.1 N HCl. The drug and marketed formulations were stable in the dissolution media used. An agitation speed of 50 rpm showed a more discriminating drug release profile than 75 rpm. The discriminating dissolution method for aceclofenac formulation is paddle at 50 rpm, 900 mL pH 6.8 phosphate buffer, greater than 80% of the label amount is released over 60 minutes.

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The objective of this investigation was to formulate ocular inserts of gatifloxacin sesquehydrate to achieve controlled drug release. Drug reservoir was prepared using hydrophilic polymers, namely polyvinyl alcohol and polyvinyl pyrrolidone. The rate controlling membrane was prepared using hydrophobic ethyl cellulose by solvent casting method. Ocular inserts were evaluated for uniformity of weight, thickness, drug content, surface pH, percentage moisture absorption, percentage moisture loss, drug excipients compatibility, in vitro release, sterility test, eye irritation, in vivo release, microbiological and stability studies. Ocular inserts complied with all the physico-chemical parameters. Drug excipients compatibility studies demonstrated no interaction between drug and polymer. The in vitro release profile of drug from ocular inserts showed controlled and prolonged release. The release data followed zero order and non-Fickian transport. Ocular inserts passed the test for sterility. Correlation between in vitro and in vivo drug release was found to be strong revealing the efficacy of the formulation. The drug was found to be effective against Staphylococcus aureus and Escherichia coli. The result of accelerated stability study revealed no significant change in drug content of promising formulation.

Statistical comparison of dissolution profiles under a variety of conditions relating to formulation characteristics, lot-to-lot, and brand-to-brand variation attracts interest of pharmaceutical scientist. The objective of this work is to apply several profile comparison approaches to the dissolution data of five-marketed aceclofenac tablet formulations. Model-independent approaches including ANOVA-based procedures, ratio test procedure, and pair wise procedure. The ratio test includes percentage, area under the curve, mean dissolution time, while the pair wise procedure includes difference factor (f1), similarity factor (f2), and Rescigno index. In the model-dependent approach, zero order, first order, Hixson-Crowell, Higuchi, and Weibull models were applied to the utilization of fit factors. All the approaches were applicable and useful. ANOVA with multiple comparison tests was found to be sensitive and discriminating for comparing the profiles. Weibull parameters were more sensitive to the difference between two release kinetic data in terms of curve shape and level.