A novel long-acting biodegradable depot formulation of anastrozole for breast cancer therapy.

The purpose of the present study was to fabricate PLGA 50:50 and PLA microspheres for controlled delivery of anastrozole. The microspheres were prepared by oil-in-water (o/w) emulsion/solvent evaporation technique and evaluated for particle size and encapsulation. The optimised formulations were studied for solid state characterization, in vitro release and pharmacokinetic studies.

A novel nanoproliposomes of lercanidipine: Development, in vitro and preclinical studies to support its effectiveness in hypertension therapy.

Aim: The aim of the present study was to develop nanoproliposomes of lercanidipine, in order to overcome its poor biopharmaceutical properties and to improve its therapeutic efficacy in treating hypertension.

Main Methods: The nanoproliposomes were prepared using a modified thin-film hydration method, and the formula was optimized by varying the ratio of lipids and the types of cryoprotectants. This optimized formulation was characterized in terms of its particle size, solid-state, drug release, in-situ absorption, in-vivo pharmacokinetics, and in-vivo anti-hypertensive activity in DOCA-salt induced hypertensive rats.

Nanomedicine of anastrozole for breast cancer: Physicochemical evaluation, in vitro cytotoxicity on BT-549 and MCF-7 cell lines and preclinical study on rat model.

Aim: Formulation and evaluation of anastrozole, an anti-cancer drug loaded in different biodegradable polymeric nanoparticles.

Materials And Methods: Different carrier systems such as poly(lactide-co-glycolide) (PLGA 50:50), poly(lactic-acid) (PLA) and poly(ε-caprolactone) (PCL) are used to prepare nanoparticles by simple emulsion technique. The surfactants polyvinyl alcohol and sodium deoxycholate were studied for their use as stabilizing agents at varying concentrations.

Role of Components in the Formation of Self-microemulsifying Drug Delivery Systems.

Pharmaceutical research is focused in designing novel drug delivery systems to improve the bioavailability of poorly water soluble drugs. Self-microemulsifying drug delivery systems, one among the lipid-based dosage forms were proven to be promising in improving the oral bioavailability of such drugs by enhancing solubility, permeability and avoiding first-pass metabolism via enhanced lymphatic transport. Further, they have been successful in avoiding both inter and intra individual variations as well as the dose disproportionality.

PEGylated liposomes of anastrozole for long-term treatment of breast cancer: in vitro and in vivo evaluation.

The aim of present study was to develop conventional and PEGylated (long circulating), liposomes containing anastrozole (ANS) for effective treatment of breast cancer. ANS is a third-generation non-steroidal aromatase inhibitor of the triazole class used for the treatment of advanced and late-stage breast cancer in post-menopausal women. Under such disease conditions the median duration of therapy should be prolonged until tumor regression ends (>31 months).

Gastroretentive pulsatile release tablets of lercanidipine HCl: development, statistical optimization, and in vitro and in vivo evaluation.

The present study was aimed at the development of gastroretentive floating pulsatile release tablets (FPRTs) of lercanidipine HCl to enhance the bioavailability and treat early morning surge in blood pressure. Immediate release core tablets containing lercanidipine HCl were prepared and optimized core tablets were compression-coated using buoyant layer containing polyethylene oxide (PEO) WSR coagulant, sodium bicarbonate, and directly compressible lactose. FPRTs were evaluated for various in vitro physicochemical parameters, drug-excipient compatibility, buoyancy, swelling, and release studies.

Transdermal delivery of lercanidipine hydrochloride: effect of chemical enhancers and ultrasound.

The effects of permeation enhancers and sonophoresis on the transdermal permeation of lercanidipine hydrochloride (LRDP) across mouse skin were investigated. Parameters including drug solubility, partition coefficient, drug degradation and drug permeation in skin were determined. Tween-20, dimethyl formamide, propylene glycol, poly ethylene glycol (5% v/v) and different concentration of ethanol were used for permeation enhancement.

Supercritical fluid technology: concepts and pharmaceutical applications.

Unlabelled: In light of environmental apprehension, supercritical fluid technology (SFT) exhibits excellent opportunities to accomplish key objectives in the drug delivery sector. Supercritical fluid extraction using carbon dioxide (CO(2)) has been recognized as a green technology. It is a clean and versatile solvent with gas-like diffusivity and liquid-like density in the supercritical phase, which has provided an excellent alternative to the use of chemical solvents.

Regulatory aspects of pharmaceuticals' exports in gulf cooperation council countries.

The Gulf cooperation council (GCC) region is considered as "Emerging market" for pharmaceutical export and bilateral trade. The understanding of the regulatory requirements of this region can be beneficial for pharmaceutical export. Some incidents of the year 2008-09, like recession or economic slowdown in highly well-off and regulated market of the EU and US, raised the demand for alternate destinations for business.

Sustained release optimized formulation of anastrozole-loaded chitosan microspheres: in vitro and in vivo evaluation.

The purpose of this study was to develop sustained release formulation of anastrozole-loaded chitosan microspheres for treatment of breast cancer. Chitosan microspheres cross-linked with two different cross-linking agents viz, tripolyphosphate (TPP) and glutaraldehyde (GA) were prepared using single emulsion (w/o) method. A reverse phase HPLC method was developed and used for quantification of drug in microspheres and rat plasma.

Novel liquid chromatographic method for simultaneous estimation of pioglitazone and glimepiride in rat plasma by solid phase extraction: application to preclinical pharmacokinetic studies.

The need for a reliable bioanalytical method is of primary importance during preclinical studies. The aim of the present study was simultaneous determination of pioglitazone (CAS 111025-46-8) (PIO) and glimepiride (CAS 93479-97-1) (GLM) in plasma of rats. A high-performance liquid chromatographic method has been developed and validated using C18 column and UV detector.

Erythrocytes as carrier for prednisolone: in vitro and in vivo evaluation.

Resealed erythrocytes, as drug delivery system has tremendous potential to achieve site specificity and prolonged release of drug thereby enhancing therapeutic index and patient compliance. In the present investigation erythrocytes obtained from healthy volunteers were loaded with prednisolone using preswell dilution and dilution technique with two different cross-linking agents, glutaraldehyde and dimethylsulphoxide. Carrier erythrocytes, having acceptable loading parameters showed increased percentage drug content with the addition of cross-linking agents.

Controlled release polymeric ocular delivery of acyclovir.

The aim of the present study was to formulate and evaluate controlled release polymeric ocular delivery of acyclovir. Reservoir-type ocular inserts were fabricated by sandwiching hydroxypropyl methylcellulose (HPMC) matrix film containing acyclovir between two rate controlling membranes of cellulose acetate phthalate (CAP). The solubility and dissolution rate of poorly soluble acyclovir was enhanced by preparing binary systems with beta-cyclodextrin and then incorporated into HPMC matrix.

Isolation and characterization of some potential impurities in ropinirole hydrochloride.

Three impurities in ropinirole hydrochloride drug substance at levels approximately 0.06-0.15% were detected by reverse-phase high performance liquid chromatography (HPLC).