Current Issue : October - December Volume : 2015 Issue Number : 4 Articles : 8 Articles
Arthritis patients requires long-term therapy, the recent trend is to use of traditional medications in combination with allopathic drug. The objective of treatment was to suppress all inflammation and prevent joint damage. The purpose of this study was to design and development of transdermal drug delivery system (TDDS) for arthritis by using boswellic acid as a drug and evaluation of in-vivo effects. Transdermal patches were prepared by solvent evaporation method. The 32 box-behnken design was applied for the optimization of process variables. The factors involved polymer, plasticizer, penetration enhancer concentration and selected responses were flux and tensile strength. Patch was also evaluated for ex-vivo skin permeation study; in-vivo carrageenan induced paw edema and also compared with conventional NSAID patch. TDDS patch was optimized with statistical design, tensile strength was found to in the range 0.3860-0.9956 (kg/cm2) and flux 15.498-20.217 (μg/cm2/hr). Polymer, plasticizer and penetration enhancer concentration showed significantly effect on tensile strength and flux. Based on these result optimized patch subjected to ex vivo study and which shown flux 15.86 μg/cm2/hr, pharmacodynamic study showed significant reduction in the paw volume after 4th hour of inflammation induction comparable to that of NSAID patch. It was concluded that transdermal delivery of boswellic acid overcomes the main disadvantage of oral delivery which is gastric irritation and the anti-inflammatory effect thus produced via peripheral administration involves inhibition of leukotriene and other endogenous substances which are key players in pain and inflammation....
Valsartan is an angiotensin II antagonist belonging to class II BCS, its low aqueous solubility leads to high variability in its absorption after oral administration. The aim of this study was to improve the dissolution of Valsartan through the development of solid self nano-emulsifying drug delivery systems (S-SNEDDS) using melting technique. For this purpose, four different oils namely; Capmul® MCM, Labrafil® M1944, Capryol™ 90 and Labrafac® PG were used together with Cremophor® RH 40 as surfactant which was screened previously according to its ability to emulsify the oil. Solidifying agents namely; PEG 4000 and Pluronic® F-68 were screened according their ability to solidify the different oil-surfactant mixtures. The effect of solidifying agent type on the in-vitro valsartan dissolution (Q5min) was studied. Characterization of the prepared S-SNEDDS was also carried out via content uniformity, DSC and FT-IR. Formula S6 prepared using Labrafil® M 1944 as oil and Cremophore® RH40 as surfactant in a ratio of (1:2) together with Pluronic® F68 (40% w/w) as solidifying agent showed promising results in terms of dissolution studies where 58.39%±1.88 of valsartan was dissolved compared to the market Disartan 80 mg capsules (13.43%±0.57). Content uniformity complied with the Pharmacopoeial limit. The disappearance of endothermic valsartan peak in the DSC thermogram suggested its conversion to amorphous form within the prepared S-SNEDDS. Compatibility of valsartan with the different excipients was confirmed using FT-IR. Therefore, S-SNEDDS could be considered as a promising approach to improve the dissolution of the poorly water soluble, valsartan....
The present formulation study of paclitaxel was performed as an attempt to prepare BSA nanoparticulate drug delivery system using desolvation method with spray drying and performance of these formulations was evaluated. From the experimental results it was concluded that: Bovine serum albumin (BSA) is an ideal carrier for preparing nanoparticles of paclitaxel. The use of acetone consistently gave smaller particles as compared to ethanol for all BSA concentrations. Desolvated BSA nanoparticles have the stability problem hence glutaraldehyde (GTA) is used as cross-linking agent for the production of stable nanoparticles. GTA also affect the entrapment efficiency and release rate but had no influence on particle size. Tween 80 is non-ionic surfactant used as dispersing agent to form stable nanoparticles....
The main objective of the present investigation was to formulate and evaluate the aceclofenac nanocapsules for the controlled release of drug to control pain and its associated disease conditions. The nanocapsules of aceclofenac were prepared by deposition of (PLGA) polymer at the O/W interface following acetone displacement from the oily nanodroplets. In this study, different concentrations of PLGA were used (ANC1-ANC5) and selected the best formulation based on its in-vitro drug release profile. The drug content for the aceclofenac nanocapsules varied from 76.8±0.13% to 99.8±0.51%. The entrapment efficiencies were found to be minimum and maximum of 70.99±0.21% and 90.39±0.11%, particle size varied from 210.4±0.23 nm to 325.6±0.62 nm, zeta potential values were in negative and increased from -21.6±0.12 mV to-15.9±0.37 mV. The in-vitro drug release profile of aceclofenac nanocapsules containing 200 mg of PLGA (ANC4) exhibited a desired drug release of 98.41±0.16 at the end of 24 hrs. The study demonstrated the successful preparation of controlled release nanocapsules of aceclofenac....
The objective of the present investigation was to develop and evaluate microemulsion based gel for the topical delivery of diclofenac sodium. The solubility of diclofenac sodium in oils, surfactants and cosurfactants was evaluated to identify components of microemulsion. The ternary diagram was plotted to identify the area of microemulsion existence. The 32 full experimental design was adopted to optimize the amount of Smix (mixture of surfactant and cosurfactant) (X1) and concentration of gelling agent (X2) in the microemulsion based gel. The formulations were assessed for % in-vitro drug release (Y1) and viscosity (cp) (Y2). The microemulsion containing 10% oil, 55% Smix, 35% water and 1.75% carbopol 980 was selected as optimized batch. The formulated microemulsion exhibits droplet size 192.2 nm, zeta potential -0.00856. The optimized microemulsion and microemulsion based gel was evaluated for their droplet size, zeta potential and physical appearance, pH, viscosity, globule size, drug content, spreadability, in-vitro and ex-vivo drug release, anti-inflammatory activity, stability study respectively. The formulated microemulsion exhibited droplet size 192.2 nm, zeta potential -0.00856 and optimized gel formulation appear as milky white, exhibits globule size 411.5 nm, pH 6.39±0.8, viscosity 14194 cp, % drug release 91.87±1.3, % drug content 98.23±1.2 respectively. The optimized microemulsion based gel did not show any signs skin irritation and exhibits anti-inflammatory study as effective as marketed gel (Voveron gel). In conclusion the microemulsion based gel may be used as an alternative for the transdermal delivery of diclofenac sodium....
Erythromycin is a bacteriostatic macrolide antibiotic which is effective against skin and the upper respiratory tract infections caused by Gram-positive bacteria. In this study, erythromycin was formulated into PLGA nanoparticles via emulsion solvent evaporation method. Entrapment efficiency of erythromycin in PLGA nanoparticles was determined microbiologically. The effect of PLGA amount, PLGA type, organic solvent, sonication probe diameter, sonication time, organic phase: aqueous phase ratio as well as effect of PVA percent on microbiologically determined entrapment efficiency was assessed. The results showed that microbiologically determined entrapment efficiency was significantly enhanced after optimizing different parameters to reach 51.1±0.68% for the optimum formula (F10). The size of the nanoparticles produced by optimal formulation observed from SEM micrographs was around 100 nm with narrow particle size distribution. The optimized formula was found to be more biologically effective then the free drug....
Controlled release local delivery systems offer advantage compared to systemic dosage forms for periodontitis. The objective of this research was to design and evaluated sustained release dental implants containing doxycycline hyclate. Doxycycline hyclate (DOX) is an antimicrobial agent that is effective against periodontal pathogens in 100 mg oral dose. Attention has been drawn toward the formulation of DOX in a reduced dose dental implant (0.6 mg / 0.14 cm2) that can support inhibitory concentration of DOX and can be placed into the periodontal pocket for at least one week. Dental implants were prepared by solvent casting technique, using chitosan either alone or co-polymered with; Eudragit L100-55, PVP K30, HPMC-K4M, HPC or HPMC-E4 and glycerin as plasticizers; The dental implants were evaluated for physicochemical and mechanical properties, in-vitro release and anti-microbial activity to determine the optimum formulation. The selected dental implant (F#1 containing both DOX and chitosan 1% W/V) showed good anti-microbiological activity against Staphylococcus aureus and Escherichia coli at this reduced dose. The study suggested that chitosan based dental implant of DOX is a promising delivery system for periodontitis treatment....
The aim of the present study was to prepare and evaluate niosomes using clopidogrel bisulphate as a model drug. The clopidogrel bisulphate niosomes were prepared by using span 60 with different proportions and cholesterol by two methods such as thin film hydration method and ether injection method. The prepared niosomes were characterized for drug entrapment efficiency, particle size, in-vitro studies and drug release kinetics. The preformulation studies such as solubility analysis, drug-excipients compatibility studies were performed. The niosomes of thin film hydration method, formulation TF-8 showed highest entrapment efficiency (80.1%) than the ether injection method formulation EF-8 showed little increase (46.55%). In-vitro release studies showed that the percentage amount of free drug release was 70.37% for TF-1 and 98.11% for EF-1 within 8 hrs. The microscopic examination of the prepared niosomes revealed spherical small unilamellar vesicles of 169.4, 170.3 and 175.4 for TF1, TF3 and TF6. The drug release kinetic data was best fitted for Koresmeyer-Peppa’s model exhibiting regression, r2 = 0.994 and showed good linearity. The clopidogrel bisulphate was successfully encapsulated into niosomes Span 60 (1:2:1) vesicles prepared by thin film hydration method showed highest entrapment efficiency and less % in-vitro drug release than the ether injection method....
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