FORMULATION, DEVELOPMENT AND CHARACTERIZATION OF SOLID LIPID NANOPARTICLES OF GEMCITABINE HYDROCHLORIDE

Gemcitabine Hydrochloride is a BCS class III drug of choice in the treatment of cancer, as a single or in combination chemotherapy. However, its bioavailability is a major concern due to its short half-life. Solid lipid nanoparticles (SLN) of Gemcitabine Hydrochloride were prepared to enhance its bioavailability, hence anticancer activity. The Quality by Design approach was applied for the formulation of SLN. The Randomized 32 factorial design was used with responses of particle size and % entrapment efficiency (% EE). The optimized batch of Gemcitabine Hydrochloride loaded SLN containing 1gm of GMS as solid lipid, 1gm of Tween80: Sodium Taurocholate as surfactant:co-surfactant and 5mg of Gemcitabine Hydrochloride was prepared by high shear homogenization method followed by Probe sonication for 15min to form nanoparticulate SLN dispersion. The Optimized batch of Gemcitabine Hydrochloride loaded SLN that exhausted mean particle size of 126.1nm, zeta potential -28.6 mV and % EE 74.83% respectively. SEM studies revealed three-dimensional nature of SLN with a slightly rough surface. DSC, results exhibited entrapment of Gemcitabine Hydrochloride in SLN. The optimized batch of SLN was evaluated for in-vitro % drug release using cellulose membrane dialysis bags for 24hrs and showed 63.13% CDR at 24 hrs. Anticancer cell line studies were also performed in human lung cancer cell line (A-549). It concludes that Gemcitabine Hydrochloride loaded Solid lipid Nanoparticles was successfully formulated and evaluated to sustain the drug release by bypassing the first pass metabolism. Key words: Gemcitabine Hydrochloride, SLN, QbD, High shear homogenization, anticancer activity.Â

FORMULATION AND EVALUATION OF BILAYER TABLETS OF PROPRANOLOL HYDROCHLORIDE

The purpose of this study is to prepare a bilayer tablet of Propranolol HCl using Wet granulation technology and to formulate optimized formulation. Propranolol HCl, a nonselective β-adrenergic blocker which is the best drug candidate to formulate in to bilayer tablets fast release of drug from immediate release layer can give rapid onset of action which will help which will help to reduce Blood pressure within short period of time while maintenance dose of Propranolol HCl will maintain plasma concentration within therapeutic range for 12hrs  having short half-life (3-5 hr) and first pass metabolism favors for sustained release dosage form. The tablets were prepared by wet granulation method. Hydrophobic matrix materials such as ethyl cellulose were used, which can release the drug up to 12 hrs in predetermined rate. Binder used was Starch paste (10%).The influence of hydrophobic polymer and granulation technique was studied. In this study, a bilayer tablet was prepared which contains an immediate release portion layer and sustained release portion.  Ethyl cellulose were used as in alone, for Sustained release and Superdisintegrant Cross Povidone for immediate release used. The bilayer tablets were characterized by Calibration Curve, Calculation of Dose, Bulk Density, Tapped density, Angle of repose, Carr’s Index, Hausner’s ratio, Weight Variation, Hardness, Friability, Thickness, Drug Content and In-vitro dissolution profile. The granules showed satisfactory flow properties and compressibility. Best Formulation F3 [Drug + Ethylcellulose (1:3)] showed High % drug release 87.40% release, high drug content, high hardness and friability. Hence, it was found better than F1 and F2 so F3 is the best formulation. Keywords: Propranolol Hydrochloride, Ethylcellulose, Bilayer Tablets