International Journal of Drug Delivery
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Preparation and Evaluation of Curcumin Invasomes
Get PDFCurcumin has poor aqueous solubility and has bioavailability problems. Hence in the present study the solubility of curcumin was increased by complexing with cyclodextrin (CD) and Hydroxy propyl β cyclodextrin(HPβCD). This complex was incorporated in to invasomes and then into HPMC gel to prepare as a transdermal formulation. Curcumin cyclodextrin complexes were prepared by physical mixture and co-precipitation method. Different formulations of invasomes containing 0.5, 1.0, 1.5 % of limonene, fenchone, nerolidol were prepared using mechanical dispersion technique. Invasomes were characterized for vesicular size, surface morphology, zeta potential, entrapment efficiency and percutaneous permeation. Formulations CHL1 and CHL2 were optimized for further studies. It was found in the study that complexation with HPβCD in 1:2 proportion prepared by co-precipitation method was found to bind 90% of curcumin. Invasomal preparation with 0.5% limonene, 4% ethanol was found to enhance permeation by 8.11 times the control. In vivo diffusion studies were conducted using franz diffusion cell, ex vivo skin permeation studies of CHL1 using rat abdominal skin showed cumulative drug permeated (Q24) of 70.32 µg/cm2, steady state transdermal flux of 3.344 µg/cm2/hr-1, permeability coefficient of 5.35 cm/hr and lag time of 1 hr when compared with control formulation. From the results it was concluded that the solubility of curcumin was increased by complexing with HPβCD and invasomal preparation with 0.5% limonene has improved the permeation through the skin
Comparison of different nano biocomposites of neomycin with marketed ointment by in-vitro and in-vivo evaluations
Get PDFNano drug delivery systems have rapid onset of action with enhanced therapeutic efficacy, decreased dose of the drug and decreased toxic effects when compared to conventional drug delivery systems. Hence neomycin is formulated into nanoparticles in order to increase the therapeutic efficacy, decrease the dose of drug and to decrease the topical dose related toxic effects. Hence the present work was aimed at the preparation of zinc nanoparticles (NP1), chitosan nanoparticles (NP2), different zinc chitosan neomycin nanoparticles (NP3,NP4,NP5,NP6,NP7,NP8) by altering the concentrations of chitosan and neomycin used in the formulation in order to optimise the composition. Nanoparticles were prepared by subjecting the nanosuspension containing the specified ingredients to stirring at 40оC for 4-5 hr. The prepared nanoparticles were evaluated for particle size and surface morphology by Transmission Electron Microscopy (TEM), mean particle size and particle size distribution by zeta sizer, percentage yield, loading efficiency, in-vitro drug release by diffusion technique and agar cup plate method and invivo wound healing activity. Among all the prepared zinc chitosan neomycin nanoparticles NP6 was found to possess maximum in-vitro drug release and antimicrobial activity. This may be due to the synergistic effect of all the ingredients i.e zinc, chitosan and neomycin present in the formulation. Hence zinc chitosan neomycin nanoparticles NP6 was subjected to in-vivo studies and compared with marketed neomycin ointment (nemozin). The wound healing was found to be more in group treated with ointment prepared with zinc chitosan neomycin nanoparticles compared to group treated with marketed neomycin ointment(nemozin) containing double the concentration of neomycin of NP6. Thus, the present work suggested that NP6 (0.2%) was found to be the best formulation of neomycin containing less than half of the concentration of neomycin of nemozin ointment(0.5%) as it shown equal invivo activity to nemozin ointment as this reduces the side effects, increases efficacy at low doses of drug compared to conventional formulations of neomycin
Development of non-invasive transdermal patch of Emblica officinalis for anti atherosclerotic activity
Get PDFThe present study was designed to formulate matrix type transdermal patches of a potent anti atherosclerotic botanical Emblica officinalis on a mercury substrate and evaluated for physicochemical parameters like thickness, % flatness, weight variation, moisture uptake, moisture content, folding endurance, elongation and drug content values. Further, in vivo drug release was also observed by HPLC in rabbit serum. Four formulations were prepared using different ratio of matrix forming polymers, plasticizer and penetration enhancers. Formulations E-1, E-2, E-3 and E-4 were composed of Ethyl cellulose (EC) and Hydroxypropyl Methylcellulose (HPMC) with the following ratios: 6:4, 7:3, 8:2 and 9:1. In vitro cumulative amounts of the permeated drug were observed 48.53, 55.46, 73.26 and 99.72% in 48 hrs from the four formulations. The release profile of the optimized formulation E-4; r2 = 0.984 (Higuchi) showed that permeation of the drug controlled by a diffusion mechanism. The cumulative amount of the permeated drug after 48hrs from E-4 was 343.95mcg/cm2. Permeability coefficient was calculated 7.16mcg/cm2/hr. Based on physicochemical and in vitro skin permeation studies, E-4 was chosen for further in vivo studies. Blood plasma concentration of E-4 after 48 hrs was 0.2914mcg/cm2. Skin permeation performance and scanning electron microscopic studies revealed that formulation E-4 was found to be better than other formulations and it was selected as the optimized formulation. The skin irritation tests showed negligible erythema and edema. The developed transdermal patches may increase the efficacy of E. officinalis for the therapy of atherosclerosis
NOVEL STRATEGY IN CONTROLLED GASTRORETENTIVE DRUG DELIVERY: IN-SITU FLOATING GEL
Get PDFAttempts are made in research and development of sustained and controlled drug delivery systems to overcome physiological and unpredictable gastric empting time (GET). Such dosage forms are useful for the drugs with ‘narrow therapeutic index'. Formation of gel depends on factors such as temperature, pH, ionic cross linking and UV irradiation, from which drug is released in controlled or sustained manner. In-situ gelling systems is prominent among other novel drug delivery systems (NDDS), due to advantages such as sustained and prolonged drug action, improved patient compliance and reduced frequency of drug administration as compared to conventional drug delivery system. These polymeric formulations are in solution form before administration and then turns to gel form when comes in contact with gastric fluids. Various natural, biodegradable, biocompatible and water soluble polymers such as pectin, gallen gum, chitosan, poly-caprolactone, xyloglucane, poly-D, L-lactic acid, pluronic F 127, carbopol, etc makes this drug delivery most acceptable and useful. In-situ gel is fabricated for both local and systemic drug delivery at specific site of action. Various evaluations are recommended for in-situ gels mostly viscosity, buoyancy, gelling capacity and dissolution studies are performed. This review presents current trends in fabrication, evaluation parameters and importance of various drugs formulated as in-situ gelling system
Development and characterization of enteric-coated salbutamol sulphate time release tablets.
Get PDFIn the present study, an attempt was made to develop immediate-release enteric-coated time release tablets of salbutamol sulphate for the treatment of nocturnal asthma. Nocturnal asthma is an asthma phenotype marked by nighttime increases in airway inflammation, airway hyper responsiveness, and expiratory airflow limitation. The occurrence of nocturnal asthma is associated with increased morbidity and inadequate asthma control, and has an important negative impact on quality of life. Formulation of enteric-coated time release tablets with suitable lag time could address the problems associated with asthma. To achieve this goal, immediate release tablets were prepared by direct compression method using superdisintegrants that contribute to the faster disintegration of tablet and thereby improved solubility of the drug. Different disintegrants like cross caramellose sodium, crospovidone and sodium starch glycolate in different concentrations (2.5 – 7.5%w/w) were tried in order to further improve disintegration time. The formulation, which showed best disintegration and dissolution profile, was coated with ethyl cellulose as inner layer and Eudragit S100 as outer enteric-coating polymer which does not dissolve at gastric pH but dissolve at intestinal pH, releasing the drug immediately in the alkaline medium. The optimized enteric-coated formulation E6 containing 2.5%w/w of Eudragit S 100 and 30%w/w of ethyl cellulose as coating system inhibited the release of the drug in 0.1 N HCl, and whereas 99.04% of drug was released in the intestinal medium. Thus, dissolution profiles indicated that E6 tablet may be better alternative in the treatment of nocturnal asthma which overcomes the problems of conventional forms
DESIGN AND IN VIVO EVALUATION OF METOPROLOL TARTRATE BILAYER FLOATING TABLETS IN HEALTHY HUMAN VOLUNTEERS
Get PDFThe aim of the present investigation was to prepare bilayer floating tablets of metoprolol tartrate using the combination of superdisintigrants, HPMC K grade polymers and natural polymers like xanthan gum and guar gum by direct compression method. Bilayer floating tablets were prepared using optimized immediate release layer and floating layer as sustained release layer. The physico-chemical characteristics of the prepared tablets were evaluated and found to be satisfactory. All the prepared batches showed in vitro buoyancy. It was observed that the tablets remained buoyant for more than 12 h. Formulation F7 was selected as best formulation based on the in vitro characteristics and used in vivo radiographic studies by adding barium sulphate. These studies revealed that the tablets remained in the stomach for 210±5.4 min (n=3) in fasting human volunteers. Based on the in vivo performance in healthy subjects, the developed bilayer floating tablets showed superior bioavailability than the marketed tablets, the drug release was up to 12 h in controlled manner. The systemic availability of the best formulation was high after administration to obtain immediate action due to the immediate release layer, from sustained release layer the drug was released in controlled manner. It can be concluded that the best formulation F7 by choosing biphasic drug release pattern in a single dosage form could improve patient compliance and ensure better disease management
Synthesis, Antifungal Activity and Molecular Docking Studies on N-(Substituted-benzylidineamine)-3- cycloalkylidine-thiosemicarbazide Derivatives
Get PDFA series of substituted N-(Benzylidineamine)-3-cycloalkylidine-thiosemicarbazide derivatives have been synthesized, characterized and evaluated for their antifungal and antibacterial activities. The newly synthesized compounds were characterized by IR, NMR, Mass and elemental analysis. All compounds were tested for antifungal and antibacterial activities. The preliminary results revealed that some of the compounds exhibited promising antifungal activities. Among the tested compounds, compound 14 (MIC 8 µg/mL) and 25 (MIC 8 µg/mL) were the most effective against C. Tropicalis. Important SAR information was also gathered. Molecular modeling investigations showed that the active compounds may interact at the active site of the fungal cytochrome P450-dependent sterol 14α- demethylase (CYP51) in the sterol biosynthesis pathway.
PREPARATION AND STATISTICAL OPTIMIZATION OF SELF NANOEMULSIFYING TABLETS OF EFAVIRENZ USING 23 FACTORIAL DESIGNS
Get PDFThe objective of the present research was to enhance the solubility of poorly water soluble antiretroviral drug i.e. efavirenz, by self nanoemulsifying drug delivery system (SNEDDS) and formulating it as tablets using 23 factorial designs. The SNEDDS were prepared using labrafac PG (15%) as oil, Tween 80 (19%) as surfactant and PEG 200 (38%) as co surfactant that yields the globule size of 142.7nm. The liquid SNEDDS were adsorbed onto aerosil which acts as carrier. The SEM of S-SNEDDS appeared as smooth-surfaced particles without any crystalline shape, indicating complete adsorption of SNEDDS. The absence of drug peak in S-SNEDDS thermogram was attributable to presence of drug in molecularly dissolved state in the vicinity of the lipid excipients. The 23 factorial designs were employed to optimize the concentration of Micro crystalline cellulose, PVP and sodium starch glycollate. The observed values were in close agreement with the predicted values thereby validating the feasibility of the optimization procedure in developing self nanoemulsifying tablets. The relative bioavailability of the S SNEDDS and pure drug were 388.49% and 95.39%, respectively. This confirms that the solubility of the drug has been increased leading to increase in the bioavailability of efavirenz
Formulation and In-Vitro Evaluation of Mucoadhesive Buccal Tablets of Atorvastatin Calcium
Get PDFThe objective of present study is to prepare buccoadhesive buccal tablets of Atorvastatin calcium (AVC-8mg) using the bioadhesive polymers Carbopol 974P (CP), Guar Gum, and Gum Ghatti as matrix forming agent and Ethyl cellulose (EC-25mg) as impermeable backing layer. The solubility studies were conducted along with PEG 4000 in different medias. Twelve formulations of mucoadhesive buccal tablets of AVC were prepared, which contain the polymers in various combinations. Tablets were prepared by direct compression method and characterized for swelling studies, % matrix erosion, surface pH, bioadhesive properties, in-vitro drug dissolution and in-vitro diffusion studies. All the formulations shows the satisfactory results in terms of bioadhesive performance. The swelling index was proportional to polymer content. The surface pH of all tablets was found to be satisfactory, close to neutral pH; the AVC released and drug diffusion from these tablets was depended on the ratio and type of the natural polymers used in the formulation. The AVC released mechanism was found to. Tablets containing CP (10%) and Guar Gum, HPMCK4M and Gum Ghatti in the ratio of 1:3 (F3, F7 and F8) shows near zero order kinetics release, with non-Fickians diffusion and followed anomalous release. The ex vivo permeation concluded that PEG 4000 enhanced the permeability of AVC from the tablets. FT-IR studies revealed that there is no interaction between drug and polymer used in the study
Antitumor and structure antioxidant activity relationship of Colchicine on Ehrlich ascites Carcinoma (EAC) in Female Mice
Get PDFColchicine has been reported to play important roles in hepatoprotection, anti-inflammation in vitro anti cancer activity. The present study was initiated to evaluate antioxidant and anti-cancer effects of colchicine (10µg/mice, i.p.) in mice after subcutaneous implantation of ehrlich ascites carcinoma (EAC) for 21 days. On the 22th day, the mice were sacrificed for the estimation of tumor growth, and biochemical parameters (glucose, insulin, alanine transaminase (ALT), aspartate transaminase (AST), alkaline phosphatase (ALP), lactate dehydrogenase (LDH), lipid peroxides (TBARS), protein thiols (Pr-SHs), reduced glutathione (GSH), superoxide dismutase (SOD), glutathione peroxidase (GPx), total cholesterol (TC), triglycerides (TG), HDL-C, LDL-C, 17β-estradiol and progesterone). The results of this study showed that administration of colchicine and 5-Flourouracil individually for 21 days to the carcinoma induced mice demonstrated a significant (P<0.01) decrease in tumor weight and a significant (P<0.01) improvement in biochemical parameters and life span compared to the EAC control mice. In addition, the results clearly suggest that colchicine induced antioxidant activity on experimental EAC control mice