Meenakshi Bajpai

Enhanced Oral Bioavailability of Efavirenz by Solid Lipid Nanoparticles: In Vitro Drug Release and Pharmacokinetics Studies

Solid lipid nanoparticle is an efficient lipid based drug delivery system which can enhance the bioavailability of poorly water soluble drugs. Efavirenz is a highly lipophilic drug from nonnucleoside inhibitor category for treatment of HIV. Present work illustrates development of an SLN formulation for Efavirenz with increased bioavailability. At first, suitable lipid component and surfactant were chosen. SLNs were prepared and analyzed for physical parameters, stability, and pharmacokinetic profile. Efavirenz loaded SLNs were formulated using Glyceryl monostearate as main lipid and Tween 80 as surfactant. ESLN-3 has shown mean particle size of 124.5 ± 3.2 nm with a PDI value of 0.234, negative zeta potential, and 86% drug entrapment. In vitro drug release study has shown 60.6–98.22% drug release in 24 h by various SLN formulations. Optimized SLNs have shown good stability at 40°C ± 2°C and 75 ± 5% relative humidity (RH) for 180 days. ESLN-3 exhibited 5.32-fold increase in peak plasma concentration (C max⁡) and 10.98-fold increase in AUC in comparison to Efavirenz suspension (ES).

Development of ibuprofen nanoliposome for transdermal delivery: Physical characterization, in vitro/in vivo studies, and anti-inflammatory activity

Objective: Ibuprofen is an established non-steroidal anti-inflammatory drug commonly used for general inflammation. However, it causes gastrointestinal troubles when administered orally, thereby decreasing patient compliance. Transdermal application of vesicular formulation of Ibuprofen will provide better patient compliance and efficacy. Methods: Six different compositions of lipid constituents have been formulated into nanovesicles using thin-film hydration method and dispersed into gel using Carbopol 934. The formulations were characterized based on physicochemical parameters using photon correlation spectroscopy, transmission electron microscopy, in vitro drug release, ex vivo skin permeation using human skin, and in vivo studies. Results: The formulation, ibuprofen liposomal gel-5 (ILG-5), had nanoliposome of smallest size (159 nm) and polydispersity index (0.331). This formulation showed moderate zeta potential and the highest encapsulation. All the formulations including IG showed a considerable amount of drug release through in vitro synthetic membrane. ILG-5 showed maximum permeation during skin permeation studies. IG showed no permeation in ex vivo settings. ILG-5 has shown the highest Cmax and AUC during in vivo permeation study. Conclusions: The present work clearly shows the superiority of nanoliposome formulation over non-vesicular formulations and that lipid composition containing 7/3/1 molar ratio of phosphatidylcholine, cholesterol, and dicetyl phosphate is optimum for nanoliposome preparations, in the cases where controlled delivery of drug is needed for a sufficient period of time.

Oral Bioavailability and Stability Study of a Self-Emulsifying Drug Delivery System (SEDDS) of Amphotericin B

Amphotericin B (AmB) is a poorly water soluble polyene antifungal antibiotic which is negligibly absorbed from the gastro intestinal tract after oral administration. The objective of this research work was to study the oral bioavailability and stability of a self-emulsifying drug delivery system (SEDDS) of amphotericin B (AmB). The SEDDS formulation consisted of glyceryl monooleate, tween 80, polyethylene glycol 400 (PEG 400) and propylene glycol and had AmB content of about 8 mg per ml. The stability of the SEDDS formulation was studied in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) in comparison to pure drug. Oral bioavailability of the SEDDS formulation was studied in rats in comparison to the pure drug. The formulation was filled in two different types of capsule shell, namely HPMC capsule and hard gelatin capsule and stability of the formulation was studied for 3 months. The SEDDS formulation resulted in a mean AUC value of 40.57µg/ml.hr with mean peak plasma concentration of 6.17µg/ml reached after 2 hours after oral administration in rats, whereas concentration of AmB in plasma was not detectable after administration of the pure drug. The formulation filled in hard gelatin capsule shell was physically and chemically stable for more than 3 months under refrigeration (4°C). The study demonstrates that SEDDS approach can be successfully utilized for oral delivery of AmB.

Patented and Approval Scenario of Nanopharmaceuticals with Relevancy to Biomedical Application, Manufacturing Procedure and Safety Aspects

BACKGROUND Nanopharmaceutical is the field that arises gradually but many challenges are also still there. This review aims to identify these challenges and give the focus on their rectification. METHODS In this paper, we memorize the safety issues, patented manufacturing procedure, applications and regulatory aspects of the nanopharmaceuticals by using the peer-reviewed research literatures. All the screened literatures described the quality content of nanopharmaceuticals with relevancy to biomedical and pharmaceutical field. RESULTS Nanopharmaceuticals have great potential to resolve the different issues such as; site specific drug delivery however, many challenges are also arising in their commercialization. In the recent years, some nanopharmaceuticals have the desired quality and safety for the public, have been approved by the regulatory agencies but this field is still a thrust area that demands a lot of attention. CONCLUSION The present review article confirms the importance of nanopharmaceuticals and impart the knowledge for making the significant approaches and strategies to overcome the manufacturing, safety, legal and regulatory issues related to nanopharmaceuticals.

DEVELOPMENT OF A SIMPLE UV - SPECTROPHOTOMETRIC ASSAY METHOD FOR SATRANI DAZOLE AND STUDY OF ITS DEGRADATION PROFILE

A simple, selective, rapid, precise, economical, reprodu cible and stability - indicating UV spectrophotometric method has been developed and validated for determination of Satranida zole in pure form and pharmaceutical dosage form. From solvent effect studies and the spectral behaviour of Satranidazole, methanol was selected as solvent . The UV spectrum was scanned between 2 0 0 to 400 nm and 318 nm was selected as maximum wavelength for absorption. Beer’s law was obeyed in the concentration range of 2 - 3 0 µg /mL . T he regression coefficient was 0.999. The method was validated for accuracy, precision, specificity and robustness, in accordance with ICH guidelines. Recovery studies gave satis factory results indicating that none of common additives and excipients or the degraded impurities interfere in the assay method. Statistical analysis proved the method was precise, repr oducible, selective, specific, and accurate for analysis of Satranidaz ole . Stability testing study includes the effect of oxidation, photolysis and susceptibility to hydrolysis across a wide range of pH values. The wide linearity range, accuracy and easy preparation of diluent imply the method is suitable for routine quantif ication of Satranidazole in the quality control of bulk forms and pharmaceutical dosage forms with high precision and accuracy.

Plumbagin analogs-synthesis, characterization, and antitubercular activity

Considering the emerging problem of drug resistance in tuberculosis, there is an urgent need of development of new analogs that are useful in curing drug resistant tuberculosis. In India, tuberculosis continues to remain one of the most pressing health problems. India is the highest tuberculosis burden country in the world, accounting one fifth of global incidence - estimated 2.0-2.5 million cases annually. In 2011, approximately 8.7 million new cases of tuberculosis and 1.4 million people die from tuberculosis each year worldwide. Current antitubercular therapies are successful against normal tuberculosis but it is not suitable for drug resistant tuberculosis. In this study Plumbagin analogs, obtained from Plumbago zeylanica (Family-Plumbaginaceae), have been synthesized. Out of the various synthesized analogs, the antitubercular activity of compound a and b was evaluated using standard H37Rv and S, H, R, and E sensitive M tuberculosis strains using LRF assay method. Compound a showed strong activity against both standard H37Rv and S, H, R and E sensitive M. tuberculosis strains as compared to standard Rifampicin. The other compounds are proved to be more active against standard H37Rv and S, H, R and E sensitive M. tuberculosis strain as compared to Rifampicin.