HME-assisted formulation of taste-masked dispersible tablets of cefpodoxime proxetil and roxithromycin.

Objectives: Antibiotics are the most commonly administered medications among pediatric patients. However most of the time, accurate dose administration to children becomes a problem due to the extremely bitter taste. Cefpodoxime proxetil (CP) and roxithromycin (ROX) are antibiotics often prescribed to the pediatric population and have a bitter taste.

Fabrication, optimization and characterization of an osmotic push-pull drug delivery system for paliperidone.

Objectives: Paliperidone is a BCS class II drug with low solubility and high permeability. It has 28% absolute oral bioavailability and an elimination half-life of 23 h. An osmotic push-pull trilayer tablet currently available on the market has achieved controlled release of a low dose over an extended time period, while avoiding the need for a loading dose.

Harmine-loaded galactosylated pluronic F68-gelucire 44/14 mixed micelles for liver targeting.

Harmine (HM), a phytoconstituent has wide range of pharmacological activities including antimicrobial, antifungal, antioxidative, and anticancer. HM has shown promising anticancer activity against liver cancer cells. However, poor aqueous solubility, multidrug pump P-gp efflux, extensive metabolism, and rapid elimination due to glucuronidation/sulfation limit clinical utility of HM.

Mapping Fusogenicity of Ciprofloxacin-Loaded Liposomes with Bacterial Cells.

The process of liposome fusion with cellular membrane plays key role in delivering encapsulated drug molecule into the cell. This process becomes very important for molecules having low permeability as they fail to reach the site of action located inside the cell. Ciprofloxacin (CIP), a broad-spectrum BCS class IV antibiotic, has poor permeability.

Chrysin-loaded folate conjugated PF127-F68 mixed micelles with enhanced oral bioavailability and anticancer activity against human breast cancer cells.

Chrysin (CH), a phytoconstituent has numerous pharmacological activities including anticancer activity. However, CH suffers from a drawback of poor aqueous solubility and in turn poor bioavailability limiting its clinical utility. In this work CH loaded folate-conjugated pluronic PF127-pluronic F68 mixed micelles were prepared with an objective to augment oral bioavailability and cytotoxicity of CH in human breast cancer cell line MCF-7 by active targeting mechanism.

Crystal engineering of lactose using electrospray technology: carrier for pulmonary drug delivery.

Context: Dry powder inhalers (DPIs) consisting of a powder mixture containing coarse carrier particles (generally lactose) and micronized drug particles are used for lung drug delivery. The effective drug delivery to the lungs depends on size and shape of carrier particles. Thus, various methods have been proposed for engineering lactose particles to enhance drug delivery to lungs.

Fabrication of electrospun nanofibres of BCS II drug for enhanced dissolution and permeation across skin.

The present work reports preparation of irbesartan (IBS) loaded nanofibre mats using electrospinning technique. The prepared nanofibres were characterized by scanning electron microscopy, Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction analysis, in vitro diffusion and ex vivo skin permeation studies. FTIR studies revealed chemical compatibility of IBS and polyvinyl pyrrolidine (PVP K-30).

Ultrasound-assisted preparation of novel ibuprofen-loaded excipient with improved compression and dissolution properties.

Context: Most of the active pharmaceutical ingredients (APIs) suffer from a drawback of poor aqueous solubility. In addition to the same, some APIs show poor tabletting behavior creating problems in formulation development. Crystal engineering can be an efficient tool in rectification of such problems associated with the APIs.

Fabrication of novel GMO/Eudragit E100 nanostructures for enhancing oral bioavailability of carvedilol.

In the present work, novel nanostructures comprising of glyceryl monooleate (GMO) and Eudragit E100 were prepared using high intensity ultrasonic homogenization. 3(2) Factorial design approach was used for optimization of nanostructures. Results of regression analysis revealed that the amount of GMO and Eudragit E100 had a drastic effect on particle size and percent entrapment efficiency.

Enhanced oral bioavailability and anticancer activity of novel curcumin loaded mixed micelles in human lung cancer cells.

Background: Curcumin has a wide range of pharmacological activities including antioxidant, anti-inflammatory, antidiabetic, antibacterial, wound healing, antiatherosclerotic, hepatoprotective and anti-carcinogenic. However, its clinical applications are limited owing to its poor aqueous solubility, multidrug pump P-gp efflux, extensive in vivo metabolism and rapid elimination due to glucuronidation/sulfation.

Purpose: The objective of the current work was to prepare novel curcumin loaded mixed micelles (CUR-MM) of Pluronic F-127 (PF127) and Gelucire® 44/14 (GL44) in order to enhance its oral bioavailability and cytotoxicity in human lung cancer cell line A549.

Potentiating antimicrobial efficacy of propolis through niosomal-based system for administration.

Background: is a multicomponent active, complex resinous substance collected by honeybees () from a variety of plant sources. This study was designed to improve the antimicrobial efficacy of propolis by engineering a niosomal-based system for topical application.

Methods: Propolis was extracted in ethanol and screened for total polyphenol content.

Exploring Microstructural Changes in Structural Analogues of Ibuprofen-Hosted In Situ Gelling System and Its Influence on Pharmaceutical Performance.

The present work explores inner structuration of in situ gelling system consisting of glyceryl monooleate (GMO) and oleic acid (OA). The system under study involves investigation of microstructural changes which are believed to govern the pharmaceutical performance of final formulation. The changes which are often termed mesophasic transformation were analysed by small angle X-ray scattering (SAXS), differential scanning calorimetry (DSC), rheology and plane polarised light (PPL) microscopy.

Liquid crystalline phase as a probe for crystal engineering of lactose: carrier for pulmonary drug delivery.

The current work was undertaken to assess suitability of liquid crystalline phase for engineering of lactose crystals and their utility as a carrier in dry powder inhalation formulations. Saturated lactose solution was poured in molten glyceryl monooleate which subsequently transformed into gel. The gel microstructure was analyzed by PPL microscopy and SAXS.

Probing influence of methodological variation on active loading of acetazolamide into nanoliposomes: biophysical, in vitro, ex vivo, in vivo and rheological investigation.

In the present work comparative evaluation of acetate and pH gradient techniques for effective drug loading in liposomes has been investigated. The acetazolamide (ACZ) loaded liposomes prepared by two methods were analyzed by vesicle size analysis, zeta potential, percent encapsulation efficiency, in vitro drug release studies and intraocular pressure lowering activity. ICH guidelines were followed for determining stability of the prepared liposomes.

Mapping ion-induced mesophasic transformation in lyotropic in situ gelling system and its correlation with pharmaceutical performance.

Purpose: To investigate influence of ion induced mesophasic transformation on pharmaceutical performance of in situ gelling system consisting of glyceryl monooleate.

Methods: The prepared system showed mesophasic transformation during its conversion from sol to gel upon controlled hydration. The process of mesophasic transformation was studied by SAXS, DSC, rheology and plane polarized light microscopy.

Rheological investigation and its correlation with permeability coefficient of drug loaded carbopol gel: influence of absorption enhancers.

Context: The present study was planned to investigate the effect of absorption enhancers on the microstructure of Losartan potassium gel and hence its influence on the diffusion of Losartan potassium across nasal mucosa.

Method: Losartan potassium loaded carbopol gel (1% w/v) with and without absorption enhancers was prepared. Polyethylene glycol (PEG) 4000 and ethanol were used as absorption enhancers.

Microstructural elucidation of self-emulsifying system: effect of chemical structure.

Purpose: Self-emulsifying systems (SES) emulsify spontaneously to produce fine oil-in-water emulsion when introduced into aqueous phase. The self-emulsification process plays an important role during formation of emulsion. The objective of current work was to understand and explore the inner structuration of SES through controlled hydration and further to study the influence of additive on the same which ultimately governs performance of final formulation in terms of droplet size.

Probing influence of mesophasic transformation on performance of self-emulsifying system: effect of ion.

Self-emulsifying systems are mixtures of oils and surfactants, ideally isotropic, sometimes including cosolvents, which emulsify under conditions of gentle agitation, similar to those which would be encountered in the gastrointestinal tract. The process of self-emulsification has remained the center of attraction for most researchers. Controlled hydration of self-emulsifying systems shows formation of an intermediate gel phase which upon rupture forms an emulsion.