DEMONSTRATION OF LYMPHATIC UPTAKE OF (6)-GINGEROL SOLID LIPID NANOPARTICLES

(6)-Gingerol, a disease modifying anti-rheumatoid drug (DMARD) agent in the treatment of Rheumatoid Arthritis is a potent inhibitor of COX-1, COX-2 activity, inhibits PGE2 production. It also inhibits the production of TNF-α by blocking the cell associated conversion of TNF precursor to mature proteins thus, halting the proliferation of synovitis. (6)-Gingerol undergo extensive phase I metabolism & underlies low systemic exposure. The aim of the present study was to overcome these limitations and formulate and evaluate Ginger extract Solid Lipid Nanoparticles to improve bioavailability by enabling lymphatic uptake. (6)-Gingerol Solid Lipid Nanoparticles were prepared by melt emulsification-homogenization method and the particle size, Zeta potential PDI and % entrapment efficiency was optimized using Box Behnken design. The optimized SLN were found to be 237nm in size, bearing -25.3mv zeta potential, 0.350 PDI and entrapment efficiency of 91.33%.  Ex vivo endocytic uptake studies (everted intestine method) revealed involvement of endocytic pathways in the uptake of Solid Lipid Nanoparticles from intestine. Thus underlining the utility of SLN for enhancement of uptake of (6)-Gingerol

Preformulation Studies of Intranasal Solid Lipid Nanoparticles of Mometasone Furoate

The objective of the present work was to prepare intranasal solid lipid nanoparticles (SLN) of mometasone furoate. Mometasone furoate is BCS class II drug having low aqueous solubility and highly sensitive to hepatic metabolism. Mometasone furoate loaded nanoparticles were prepared by high pressure homogenization technique. The preformulation studied was conducted by studying various selection criteria. Lipid was chosen on the basis of maximum solubility of the drug in lipid. Glyceryl monostearate was selected as the lipid phase which showed maximum drug solubility than other lipids. Selection of surfactant, homogenization pressure and no. of homogenization cycle was done on the basis of minimum particle size and maximum % entrapment efficiency. These results showed high entrapment efficiency and minimum particle size. Keywords: Intranasal solid lipid nanoparticles, High pressure homogenization, Glyceryl monostearate

FORMULATION DEVELOPMENT OF SUSTAINED RELEASE EPIDURAL INJECTION OF ANALGESIC DRUG

The objective of this work was to formulate and evaluate sustained release epidural injection of analgesic drug diclofenac sodium used in chronic lower back pain. The formulation composed of a thermosensitive polymer Pluronic F127 (20%) and sustained release copolymers HPMC K100M (1%) and HPMC K4M (0.5%) optimized using 32 factorial design. The formulation was found to be clear, colorless, sterile, syringeable through 18gauge, forming a stable gel at 37°C with a gel strength of 9.67g/cm. The drug release was found to be 98.13% in 72 hrs. The formulation was found to be stable at refrigerator temperature of 5°C for a month. Thus, a stable parenteral formulation was developed that can be an appropriate and convenient approach for patients requiring frequent parenteral administration, reducing recurrence of dosage and ultimately expanding patient comfort and satisfaction in case of chronic ailments

Taste masking of cefuroxime axetil by ion exchange resin complex

The antibiotic cefuroxime axetil is extremely bitter. The present study deals with development of taste-masked resinates of cefuroxime axetil using ion exchange resins. The drug resin complexation procedure was optimized with respect to drug to resin ratio and pH of medium. Taste masked complex was characterized by FTIR, DSC and XRPD studies. In vitro release studies revealed complete drug release from the complex within 120 min in 0.1N HCl solution whereas less than 5 % drug was released from taste masked complex in 60 sec in simulated salivary fluid (pH 6.2) which found to be insufficient to impart bitter taste. The taste-masked complex was then formulated into a suspension dosage form using sodium carboxymethyl cellulose as suspending agent. The suspension was evaluated for various quality control parameters and in vivo studies were carried out to check bioavailability of drug from suspension.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Formulation and in-vitro evaluation of repaglinide microspheres prepared by spray drying technique

Repaglinide is a potent second generation oral hypoglycaemic agent widely used in treatment of non insulin dependent diabetic mellitus. The objective of the present study was to develop sustained release microspheres of repaglinide using ethyl cellulose and PEG 6000 as a matrix forming polymer. Microspheres were prepared by taking various concentrations of ethyl cellulose and PEG 6000 by spray drying technique. Prepared microspheres were evaluated for process yield, drug entrapment, particle size, SEM, FTIR, DSC and in vitro drug release. Process yield and drug entrapment was 40-45 % and 90-95 %, respectively. Particle size ranged in 5-22 µm and SEM study showed spherical shape and rough surface of microspheres. FTIR study and DSC analysis revealed the stable nature and amorphous dispersion of drug in the polymer matrix. In vitro release studies indicate retardation of release upto 12 h which can control both fasting blood glucose level and postprandial blood glucose.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Development of Hot Melt Coating Technique for Taste Masking of Chloroquine Phosphate Tablets

In the present study to mask the unpleasant taste of chloroquine phosphate, hot melt coating technique was used as a taste masking tool. Hot melt coating is a solvent free technology grants rapid, additionally economical coating process with reduced risk of dissolving drug during process and provide uniform application rate of coating agent. Precirol ATO 5 was used as hot melt coating material for taste masking. Tablets were prepared by wet granulation method and coated using hot melt coating technique. Coated tablets exhibited good uniformity of drug content. Amount of drug release from all batches were evaluated. Taste evaluation of hot melt coated tablets was done by using electronic tongue.PrecirolATO5 was found to be a better taste masking agent when used by hot melt coating technique. Keywords: Precirol ATO 5, Hot melt coating, taste masking

Dissolution Improvement of Poorly Water Soluble Drug Valsartan and Improving Flow Properties of Solid Dispersion

The aim of the present investigation is to improve the dissolution of poorly water soluble drug valsartan by preparing solid dispersions and also to evaluate the effect of different inert carriers on flow properties of solid dispersion. Valsartan is a poorly soluble drug useful in the treatment of hypertension. Absorption window of valsartan is stomach and upper part of small intestine. One possible way to improve dissolution rate is solid dispersions of the drug. The solid dispersions were prepared by solvent evaporation method using HPMC E5 LV as water soluble carrier, as use of HPMC low viscosity polymers for solid dispersion preparations were reported in literature. But film formation took place during solid dispersion formulation and was creating difficulty in releasing the drug from formulation; and those solid dispersions, were not free flowing. Thus such preparations are not useful from the formulation development point of view. So to improve the flow properties some inert material were tried like microcrystalline cellulose (MCC) and lactose. The solid dispersions were evaluated for drug content, solubility and dissolution studies. In vitro drug release of solid dispersions was studied by USP type II paddle dissolution apparatus. For the solid dispersion the solubility and dissolution of the drug increased with the increase in the carrier concentration. Probable mechanisms of improved solubility and dissolution were characterized by Differential Scanning Calorimetry (DSC), Powder X-ray Diffractometry (Powder XRD) and Scanning Electron Microscopy (SEM) of drug, physical mixture and solid dispersions. This study revealed that solid dispersions technique is promising and useful for valsartan to improve its solubility and dissolution and incorporation of inert carriers improved the flow property of solid dispersion.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Optimization of Carboxymethyl-Xyloglucan-Based Tramadol Matrix Tablets Using Simplex Centroid Mixture Design

The aim was to determine the release-modifying effect of carboxymethyl xyloglucan for oral drug delivery. Sustained release matrix tablets of tramadol HCl were prepared by wet granulation method using carboxymethyl xyloglucan as matrix forming polymer. HPMC K100M was used in a small amount to control the burst effect which is most commonly seen with natural hydrophilic polymers. A simplex centroid design with three independent variables and two dependent variables was employed to systematically optimize drug release profile. Carboxymethyl xyloglucan , HPMC K100M , and dicalcium phosphate were taken as independent variables. The dependent variables selected were percent of drug release at 2nd hour and at 8th hour . Response surface plots were developed, and optimum formulations were selected on the basis of desirability. The formulated tablets showed anomalous release mechanism and followed matrix drug release kinetics, resulting in regulated and complete release from the tablets within 8 to 10 hours. The polymer carboxymethyl xyloglucan and HPMC K100M had significant effect on drug release from the tablet (). Polynomial mathematical models, generated for various response variables using multiple regression analysis, were found to be statistically significant (). The statistical models developed for optimization were found to be valid

Formulation and Optimization of Sustained Release Tablets of Venlafaxine Resinates Using Response Surface Methodology

The aim of the current study was to design sustained release matrix tablets of venlafaxine hydrochloride using ion exchange resin with the incorporation of hydrophilic and hydrophobic polymer combinations. Venlafaxine HCl was loaded onto Indion 244 by batch method and then resinate were wet granulated with ethyl cellulose and blended with hydroxypropylmethylcellulose and compressed. A central composite design for 2 factors at 3 levels each was employed to systematically optimize drug release profile at 2 h and at 18 h. Hydroxypropylmethylcellulose and ethylcellulose were taken as the independent variables. Response surface plots and contour plots were drawn, and optimum formulations were selected by feasibility and grid searches. Resinate shows inadequate sustained release profile. Compressed matrices exhibited the anomalous release mechanism, as the value of release rate exponent (n) varied between 08109 and 08719, resulting in regulated and complete release until 20 h. Validation of optimization study, performed using five confirmatory runs, indicated very high degree of prognostic ability of response surface methodology, with mean percentage error as 1.152±1.88%. Regulated drug release study indicates that the hydrophilic and hydrophobic matrix tablets of venlafaxine resinate prepared using hydroxypropylmethylcellulose and ethylcellulose, can successfully be employed as a once-a-day oral controlled release drug delivery system