International Journal of Drug Delivery
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Impact of PLA/PEG ratios on Curcumin solubility and encapsulation efficiency, size and release behavior of Curcumin loaded poly(lactide)-poly(ethylenglycol) polymeric micelles
Get PDFCurcumin, a natural compound isolated from rhizomes of the herb Curcuma longa, is suggested as a potential therapeutic agent thanks to its multiple biological and pharmaceutical activities including anti-inflammatory, anti-oxidant, wound healing, anti-microbial and anti-cancer activities. Particularly, Curcumin has demonstrated efficacy as an anticancer agent for various kinds of cancer. However, its low aqueous solubility and bioavailability hamper its clinical application. Therefore, many drug delivery systems have been developed to overcome these limitations. In this study, by using polymeric micelles composed by poly (lactide)-poly (ethylenglycol) (PLA-PEG) copolymers, the aqueous solubility of Curcumin was increased to 0.73 mg.mL-1 compared to 0.11×10-4 mg.mL-1 of pure Curcumin. In addition, we found that the ratio of PLA/PEG has large impact on Curcumin solubility, Curcumin encapsulation efficiency, size and Curcumin release behavior of polymeric micelles. The increase in Curcumin solubility, Curcumin encapsulation efficacy and particle size but decrease in Curcumin release rate were observed when increasing the PLA/PEG ratio
Down Regulation of Plasma and Tissue Biomarkers by Homocastasterone
Get PDFHomocastasterone is a ketosteroid and a member of the brassinosteroid family of plant hormones. Earlier studies with 28-homobrasslinolide, an aldosteroid, had indicated that rat blood and tissue biochemical parameters studied were affected by this compound, resulting in altered homeostasis and cellular phosphorylation status, rendering this plant oxysterol inappropriate for high energy related work activities. The use of the ketosteroid in this study presents evidence for renormalization of elevated plasma lipid content in diabetic rat, antiglycemic potency, increase in liver glycogen and glucose level and diminished ALT and AST enzyme activities. A role for this ketosteroid in rat liver gluconeogenesis and in lipid homeostasis is suggested while the aldo and keto forms regulated glucose homeostasis in the rat. The observed differences in the effects of homobrasslinolide and homocastasterone as exogenous oxysterols on normal and diabetic rat plasma lipid level suggests the possibility of differential influence by endogenous aldo and keto oxycholesterol forms on glucose and lipid homeostasis in mammalian physiology
Simple and sensitive method development and validation of Econazole in human plasma by RP-HPLC
Get PDFA simple and accurate method was developed for the validation of the Econazole using Fluconazole as internal standard with short time of 10 minutes .Optimization of chromatography technique was used during the preparation of this analysis. The method carried out using reversed phase of HPLC. Chromatography using Phenomenex Luna C18 Column (250mm x 4.6mm i.d, 5µm) as the stationary phase and mobile phase of solvent A and B of 0.5% Triethylamine at pH 6.5 and Acetonitrile at pH 3.5. Wavelength was fixed at 260nm and flow rate at 0.6mL/min. Validation studies was achieved by using the fundamental parameters, including accuracy, precision, selectivity, sensitivity, linearity and range, stability studies, limit of detection (LOD) and limit of quantitation (LOQ). Retention time obtained for Econazole and Fluconazole are 7.7 minutes and 5.18 minutes. It shows recovery at 93.5% which is more precise and accurate compared to the other Econazole method. Hence, a simple and accurate method of validation of Econazole in drug free plasma was developed and validated
Targeted drug delivery system:- formulation and evaluation of chitosan nanospheres containing doxorubicin hydrochloride
Get PDFA chitosan molecule form self-assembled nanoparticles that can encapsulate a quantity of drugs and deliver them to a specific site. Chemical attachment of drug to chitosan throughout the functional linker has possibility to produce useful prodrugs, exhibiting biological activity at target site. In vivo residence time of the dosage form in the gastrointestinal tract and bioavailability of various drugs increases by mucoadhesive and absorption enhancement properties of chitosan. Antitumour activity of doxorubicin(DOX)-incorporated nanoparticles in vitro on DOX- resistant C6 glioma cells. Nanoparticles showed increased cytotoxicity compared to DOX alone. These results suggest that doxorubicin (DOX) was unable to penetrate into cells and did not effectively inhibit cell proliferation. In contrast, nanoparticles can penetrate into cells and effectively inhibit cell proliferation. There are 3 batches of drug loaded nanospheres in which 2.5mg,5mg and 10mg of DOX were loaded into nanospheres where the concentration of chitosan is 1%w/v. Anticancer drugs without targeting a specific site cause side effects. The objective of this research is to reduce side effects. HPLC device was used to quantitatively analyze amount of doxorubicin loaded in nanospheres. The result had showed concentration of anticancer drug loaded in nanospheres is directly proportional to the drug payload capacity until saturation point. The in vitro drug release studies was carried out for 48 hours to obtain a more precise result by carrying out this studies in a medium resembling our body environment such as pH7.4, 37ºC with analytical grade water for this studies. In vitro release of doxorubicin is of zero order kinetic. This shows that release is independent of the concentration of drug loaded in the nanospheres. Besides that, the graphs also show a sustained release manner, indicating these nanospheres formulation are suitable for targeting drug delivery system and for efficient treatment of cancerous cells
Development and In vivo evaluation of immediate release amlodipine besylate and nebivolol hydrochloride coated pellets using 32 full factorial design by novel liquid layering technology
Get PDFThe aim of the present investigation was to development of immediate release liquid coated pellets of poorly soluble drugs Amlodipine besylate (AMD) and Nebivolol HCl (NBV) by novel liquid layering technology to enhance solubility and bioavailability with HPC-EF as hydrophilic polymer and PVP K 30 as binder. A 32 full factorial design was employed to optimize the formulation of pellets. In order to optimize formulations, two polymers HPC-EF and PVP K 30 as factors and amount of polymers (three different concentrations), were taken as independent variables. All the formulations were evaluated for particle size, friability, moisture content, drug content, in vitro dissolution studies and in vivo bioavailability studies. All the formulations were found uniform with respect to all evaluation parameters. The optimized formulation (F5) showed highest % of drug release 99.59 by the end of 8 min for AMD and 99.21 % of drug release for NBV, when compared with the marketed product (NEBISTAR-AM) the percentage of AMD and NBV was 83.91 and 82.67 respectively within 8 min, by using 4% of HPC-EF and 1% of PVP K 30. SEM confirmed that F5 was spherical in shape with a smooth surface. In vivo studies indicated significant difference in the bioavailability between AMD and NBV coated pellets with pure drug. Clinical data confirmed that the optimized formulation (F5) by choosing immediate release drug coated pellet technology by liquid layering method could improve patient compliance and ensure better disease management when compared with the marketed product.
Efficacy and duration of analgesia from a sustained-release lidocaine sheet in humans
Get PDFBACKGROUNDWe have synthesized a sustained-releaselidocaine sheet (SRLS) and injectable sustained-release lidocaine particles(SRLP) using biodegradable polymers. In the present study, we performed anexploratory first clinical trial of the SRLS in healthy volunteers as a preludeto patient administration. This trial is meant as an initial intervention inultimately developing and refining the SRLP. METHODSWe evaluated the intensity and duration ofanalgesia of the SRLS compared with 8% lidocaine spray. In Protocol 1, weapplied the SRLS piece to the mucous membrane of the nasal vestibule. Weexamined the local pain threshold over 72 h after administration, and removedthe SRLS after 72 h. Individuals that finished Protocol 1 underwent Protocol 2,in which we applied 8% lidocaine spray. RESULTSTwelve volunteers were enrolled and seven ofthese volunteers finished Protocol 1. All seven individuals who completedProtocol 1 also completed Protocol 2. The mean pain thresholds were 32 g, 78 g,90 g, 90 g, 87 g, and 87 g at pre-administration and 4 h, 10 h, 24 h, 48 h, and72 h after administration, respectively, in Protocol 1, and 36 g, 85 g, 49 g,and 33 g at pre-administration and 15 min, 2 h, and 4 h, respectively, inProtocol 2. CONCLUSIONA sustained-release lidocaine usingbiodegradable polymers was applied as a sheet in humans for the first time inthe world. It maintained significant analgesia for 72 h without majortoxicities. Furthermore, degree of analgesia provided by the SRLS throughoutthe entire study was similar to that provided by the 8% lidocaine spray. It may suitable for management ofpostoperative pain especially in outpatients
Formulation and Evaluation of Anti-Ulcer Floating Tablet Using Swellable Polymers
Get PDFPresent study involves the formulation and evaluation of floating tablets Ranitidine hydrochloride by direct compression method by using HPMC K4M, HPMC K100M as a synthetic polymers and Gellan Gum (low acyl) as a natural polymer with addition of sodium bicarbonate and citric acid as effervescent agent. The physicochemical compatibility of the drug and the polymers was studied by infrared spectroscopy and differential scanning calorimetry. The results suggested that drug and the polymers were physicochemically compatible with each other. The effect of synthetic and natural polymers on the drug release and floating properties of tablet were investigated. Formulation was optimized on the basis of pre compression and post compression parameters, floating lag time, total floating time and in vitro drug release study was carried out. The floating lag time, dissolution studies indicated that formulation F11 with drug: polymer ratio 5:4 exhibited sustained release of drug and followed Korsemeyer Peppas kinetics. Natural polymer (Gellan Gum) showed better results for sustained drug release properties than synthetic polymer. The floating lag time was found to be increase significantly with increase in concentration of polymer and drug release was found to decrease with increase concentration of polymers
FABRICATION AND CHARACTERIZATION OF ETOPOSIDE LOADED MAGNETIC POLYMERIC MICROPARTICLES
Get PDFThe purpose of this study is to develop a targeted drug carrier system. Magnetic poly (ε-caprolactone) (PCL) microspheres were prepared using classical oil-in-water solvent evaporation method by loading magnetite nanoparticles and anticancer drug etoposide. The prepared magnetic microspheres were smooth, free flowing, individual and homogenous in nature. Fourier transformed infrared spectroscopy studies revealed the absence of any potential incompatibility of drug with other excipients. DSC studies were conducted to study the state of etoposide in the formulation. Further the magnetic microspheres were characterized for entrapment efficiency, drug loading, invitro release studies and subjected to particle size analysis and scanning electron microscopy. The magnetite nanoparticles were well dispersed in polymer matrix, which are responsible for magnetic response. The magnetic property of the prepared microspheres was measured by using vibrating sample magnetometer. The amount of magnetite in the formulation was estimated quantitatively by atomic absorption spectroscopy which was about 31.5%. The experimental results proved that the magnetic microspheres exhibited superparamagnetic behavior and the saturation magnetization was 7.26 emu/g. The optimized formulations exhibited a narrow size distribution which were below 10 μm and are evident from SEM analysis. Formulation batches prepared with drug/polymer ratio 1:10 showed a maximum encapsulation efficiency and the invitro release profile in phosphate buffer (pH 7.4) solution showed an extended release of etoposide up to 76.25% at the end of 21 day. Histopathological studies proved that the etoposide loaded magnetic microspheres were nontoxic and safe
Ternary Blends of some Hydrophilic and Hydrophobic Polymers in Colon Targeted Delivery of Metronidazole
Get PDFMatrix tablets were prepared using blends of xanthan gum (XG), Guar gum (GG) and ethylcellulose (EC). The polymers were combined using six different ratios; 1:1:1, 1:2:1, 1:2:2, 2:2:1, 2:1:2 and 2:1:1 to produce formulations XG1GG1EC1, XG1GG2EC1, XG1GG2EC2, XG2GG2EC1. XG2GG1EC2 and XG2GG1EC1 respectively. Metronidazole was used as the model drug. The ability of the prepared matrices to target drug release predominantly at the colon under the influence of colonic bacteria was evaluated using the dissolution medium containing 4 % caecal content. Our results show that, optimum drug release was observed with formulations XG2GG2EC1 and XG2GG1EC1 with Cmax of 60 and 76 % respectively. Significant difference (P<0.05) was observed between drug release in dissolution medium with and without rat caecal contents for the batches of Metronidazole tablets. Formulations (XG2GG2EC1 and XG2GG1EC1) followed Higuchi square roots kinetics ( r2 =0.9942) via fickian diffusion ( n < 0.45 ) and Korsemeyer model (r2 = 0.9939) via non – fickian diffusion (n > 0.45) respectively. Key Words; matrix.guar, xanthan, ethylcellulose, metronidazole, colon deliver
Development and Statistical optimization of mucoadhesive drug delivery system of famotidine using Hibiscus esculentus polysaccharide
Get PDFThe presentstudy was aimed to formulate and evaluate oral mucoadhesive drug deliverysystem of purified Hibiscus esculentusL polysaccharide (HEP) using famotidine as model drug. A centralcomposite design for 2 factors at 3 levels each was employed to evaluate theeffect of critical variables i.e. concentration of HEP and PVP K30 on drugrelease and mucoadhesive properties of the formulated tablets. FT-IRspectroscopy and Differential Scanning Calorimetry was carried out to evaluatedrug polymer interaction. Formulated tablets were evaluated for physicalproperties, drug release characteristic and physical stability. Ex-vivo mucoadhesion study using goatgastric mucosa was carried out to ascertain the mucoadhesion potential offormulated tablets.The responsesurface analysis clearly indicated the dominating effect of HEP on mucoadhesivestrength, mucoadhesion time and dissolution half life, while PVP K30 has anadditive effect on all afore mentioned responses. The drug release from thematrix tablets was highly affected by the concentration of release retardantspolysaccharide. The kinetics of drug release was found to be first order in lowconcentration but with increase in polymer concentration the release patternshifted towards zero order and is governed by both Higuchi and Hixson-Crowelequation indicating a coupling effect of diffusion and erosion. The result ofthe study suggests that, HEP can be optimistically explored as excellentmucoadhesive agent with controlled release characteristics