International Journal of Drug Delivery
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Enhancement of Solubility of Artemisinin and Curcumin by Co-Solvency Approach for Application in Parenteral Drug Delivery System
Get PDFThe aim of present study was to enhance solubility of poorly soluble antimalarial drugs, Artemisinin and Curcumin by adopting Co-solvency approach and to develop parenteral aqueous injectable solution. Solubility enhancement of both drugs was achieved using co-solvency approach. The parenteral injection was prepared by using a ternary co-solvent system which comprised of benzyl alcohol, PEG 400 and tween 80 (as surfactant). Solubility of Artemisinin and Curcumin was found to be higher in benzyl alcohol and PEG 400. Co-solvent system comprising of benzyl alcohol, PEG 400 and tween 80 in volume fraction of 0.3, 0.9 and 0.2 respectively showed the minimum required solubility of Artemisinin (90 mg per ml) and Curcumin (180 mg per ml). The parenteral injectable formulation was characterized for pH, clarity, viscosity, osmolarity and sterility and the stated parameters were found in acceptable range. In-vitro erythrocyte toxicity study showed that intravenous administration of optimized formulation will be safe. In-vitro antimalarial assay indicated that efficacy of artemisinin and curcumin parenteral formulation was greater than quinine and combination of Artemether and Lumefantrine. Stability study of the optimized batch showed no change in physical and chemical characteristics. Based on study, one can conclude that Artemisinin and Curcumin can be successfully formulated as parenteral injectable formulation by co-solvency approach for the effective treatment of malarial infectio
A DESCRIPTIVE REVIEW ON VARIOUS LIPIDS AND TECHNIQUES USED IN FORMULATION OF SOLID LIPID NANOPARTICLES
Get PDFSolid lipid nanopaticles (SLNs) emerged in early 1990s as a next-generation drug delivery system, an alternative to traditional colloidal carriers like liposomes, polymeric nanoparticles, emulsions etc. Their size range is between 1 to 1000 nm and their biodegradable and bioacceptable nature make them less toxic and thus better suited to patients. SLNs have got potential applications in pharmaceutical field, cosmetics, clinical medicine and other allied sciences. Presently, formulation scientists have been focusing on SLNs as colloidal drug carriers for incorporating hydrophilic as well as lipophilic drugs. The ability to incorporate drugs into nanocarriers offers a new prototype in drug delivery which can be used for drug targeting. They hold great promise for reaching the goal of controlled and site specific drug delivery. Furthermore, SLNs have got advantage of being introduced in the body by oral, parenteral and topical routes. So the present review attempts to enlighten various lipids used in SLNs, manufacturing techniques as well as the potential applications through various routes for a variety of disorders. Furthermore, the manuscript also focuses on the fate of these lipids (constituents of SLNs) in the body and their way out (i.e. elimination)
Development and in vivo evaluation of mucoadhesive tablets of Lafutidine
Get PDFThe aim of the present work was in vitro and in vivo evaluation of mucoadhesive tablets of lafutidine to prolong the gastric residence time after oral administration. Formulations were prepared using 33 full factorial designs to explore the effects of Gum Kondagogu, Gum Olibanum and Guar Gum (as independent variables) on mucoadhesive strength, drug release and Ex vivo residence time (as dependent variables) was studied and published in the earlier research paper.In this investigation the formulated mucoadhesive tablets which was optimized through in vitro studies is selected and performed the in vivo studies on Human volunteers. The drug-polymer interaction was also studied by conducting FTIR and DSC tests. The in vitro release kinetics studies reveal that all formulations fits well with Zero order, followed by Korsmeyer-Peppas, Higuchi and the mechanism of drug release is erosion. After analysis of different evaluation parameters and drug release kinetics, formulation code F22 was selected as a promising formulation for delivery of lafutidine as a mucoadhesive Gastroretentive tablet with best mucoadhesive strength and 99.54% drug release at 12th hour. Radiological evidences suggest that, a formulated tablet was well adhered for >10 h in human stomach. The bioavailability studies of F22 containing lafutidine was carried out which exhibited increased pharmacokinetic parameters of Cmax (268±1.26), Tmax (1.30±1.23 h) and AUC0-t (1048±16.42) as compared to marketed formulations which indicates improved bioavailability of formulations.
In-vitro and in-vivo evaluation of Cimetidine loaded mucoadhesive microspheres
Get PDFIn the present research work mucoadhesive microspheres of cimetidine was prepared using ionotropic gelation technique. All the microspheres were characterized for particle size, scanning electron microscopy, FT-IR study, DSC, percentage yield, drug entrapment, stability studies and for in vitro release kinetics and found to be within the limits. Among all the formulations M12 was selected as optimized formulation based on the physicochemical and release studies.In vitro drug release study of optimized formulation M12 showed 99.12% after 12 h in a controlled manner, which is essential for anti ulcer therapy. The innovator cimetine conventional tablet showed the drug release of 96.15% within 1 h. The drug release of cimetidine optimized formulation M12 followed zero order and Higuchi kinetics indicating diffusion controlled drug release. In vivo studies revealed that the optimized formulation M12 gave the highest AUC and Tmax. The results are indicative of cimetidine as mucoadhesive microspheres for improving the oral bioavailability with controlled drug release
Preparation, characterization and evaluation of finasteride ethosomes
Get PDFThe present investigation attempted to prepare and evaluate the finasteride ethosomes for transdermal drug delivery. The ethosomal formulations were developed using different concentrations of ethanol (20-60%) and soya lecithin (1-5%). In-vitro release studies of formulation containing 30% ethanol and 3% soya lecithin showed highest % drug release (82.66%) with highest transdermal flux. The entrapment efficiency and drug content of optimized formulation were found to be 85.32% and 99.5% respectively. Scanning Electron micrographs revealed that the formed vesicles were spherical in shape with uniform size. It was also observed that concentration of the ethanol had profound influence on entrapment efficiency. The drug release from the formed vesicles was found to follow first order kinetics with higuchi diffusion mechanism. The transdermal delivery of finasteride could be potentially enhanced when they were formulated into ethosomes. This ethosomal drug delivery was found to be promising than could be a nanogel
Limonene and BEZ 235 inhibits growth of COLO-320 and HCT-116 colon cancer cells
Get PDFD-Limonene is a dietary monoterpene with significant anticancer activity against many cancer types in preclinical and clinical studies. The study is designed to investigate synergistic anticancer effects of limonene and BEZ235 combination in COLO-320 and HCT-116 colon cancer cells. Cells were treated with both the drugs alone and in combination and the effects on cell viability; cell migration and clonogenic potential were examined. Results show that both drugs exhibited dose and time dependant cytotoxicity on the cell lines tested. CompuSyn analysis of the drug combination effects revealed the strong synergistic interaction of the combination. Our results also indicate that COLO-320 cells were more sensitive for anticancer effects of the drugs than HCT-116 cells. The presence of Ras and PI3K mutations in HCT-116 cells could possibly be one of the main reasons for the observed outcome as compared to the wild type expressions of them in COLO-320 cells
In Vitro - In Vivo Evaluation Of E/R Trilayer Matrix Tablets Containing Solid Dispersion Of Atorvastatin
Get PDFInvestigation of in vitro/in vivo behaviour of extended release tablets containing solid dispersions of Atorvastatin is the focus of the present research work. Atorvastatin trilayer matrix tablets were prepared by direct compression method and consisted of middle active layer with different grades of hydroxypropylmethylcellulose (HPMC), ethyl cellulose and Carbopol 934P. Barrier layers are prepared with hydrophobic polymers carnauba wax and xanthan gum. Based on the evaluation parameters, drug dissolution profile and release order kinetics HF16 was found to be optimized formulation. The developed drug delivery system provided prolonged drug release rates over a period of 24 h. The release profile of the optimized formulation (HF16) was described by the Zero-order and best fitted to Higuchi model. FTIR confirmed that there was no chemical interaction between drug and excipients used in the formulation. . In vivo bioavailability studies were conducted for optimized formulation HF16 and reference standard. The optimized formulation of Atorvastatin trilayer matrix tablet was shown significant plasma concentration with extended release and maintained for 24 hrs with patient compliance by reducing the dosage frequency, when compared with reference standard.
Niosomal 5-Flourouracil gel for effective treatment of skin cancer; In-vitro and In-vivo evaluation
Get PDFThis study was designated to form core-enriched 5-flourouracil (5-FU) niosomes and apply it to skin as a niosomal gel for topical treatment of skin cancer. Different molar ratios of the two surfactants used namely; sorbitan monostearate (Span 60), sorbitan monolaurate (Span 20) to cholesterol were employed, in addition; sodium deoxycholate was used a co-surfactant. The drug was successfully entrapped in niosomes with entrapment efficiency reached up to 67.08 ± 2.53 mg % (w/w). The produced niosomes had particle size below 300 nm, zeta potential values between -15 ± -1.6 and -37.73 ± -2.53 mV and polydispersity index between 0.09 ± 0.06 and 0.20 ± 0.02. Transmission electron microscopy showed the formation of spherical niosomes with closed bilayer structure. Formula N8 had more than two fold increase in amount permeated compared to free drug in in-vitro permeation study. The niosomal gel formulae had better permeation parameters compared to formulae containing free drug. Niosomal gel formula composed of sodium carboxymethyle cellulose (Na CMC) had the best permeation parameters among the produced gel formulae. Histopathological studies showed that niosomal 5-FU gel was able to penetrate more readily into deep layers of skin to treat tumor as indicated by the reduction in inflammatory reaction and hemorrhage signs observed in animals treated by niosomal 5-FU gel.
Development and validation of analytical methods for the simultaneous estimation of Nimorazole and Ofloxacin in tablet dosage form
Get PDFTwo simple, rapid, accurate and precise spectrophotometric methods have been developed for simultaneous estimation of Nimorazole and Ofloxacin from tablet dosage form. Method І involves formation of ‘simultaneous equations’ at 304 nm (λ max of Nimorazole) and 287.5 nm (λ max of Ofloxacin); while Method ІІ involves, formation of ‘Absorbance ratio equation’ at 301(isoabsorptive point) and 287.5 nm (λ max of Ofloxacin) using distilled water as a solvent. The linearity was observed in the concentration range of 5 - 25 μg/ml for Nimorazole and 2 - 10 μg/ml for Ofloxacin. The results of analysis have been validated statistically and by recovery studies and were found satisfactory
Miconazole Nitrate based cubosome hydrogels for topical application
Get PDFCubosomes are discrete, sub-micron, nano-structured particles of bicontinuous cubic liquid crystalline phase. Cubosomes consist of honeycombed (cavernous) structures separating two internal aqueous channels and a large interfacial area. They are the biocompatible novel approach for the drug delivery system. The controlled release application of these nanoparticles is of a great significance in cosmeceutical and pharmaceutical fields. The present study is concerned with the design and evaluation of a novel nano-particulate system; cubosomes, loaded with miconazole nitrate (MN); which is used as antifungal agent. Cubosome dispersions were formulated by emulsification technique using different concentrations of a lipid phase monoolein and the nonionic surfactant, Poloxamer 407. The prepared cubosomal dispersions were characterized regarding dimensional distribution, particle size, and in vitro drug release. The optimum formulae were incorporated in a CMC or HPMC based hydrogels, to form cubosomal hydrogels (cubogels). The cubogels were characterized regarding in vitro release of (MN), viscosity and pH. A comparison between the cubogels and a commercially available product, Miconaz® cream, was carried out to judge their efficacy. The drug release from the commercial preparation was lower than all the prepared nano-emulsion based gel formulations. G1 and G8 showed highest drug release percent (100%) after 8 hours, in contrast the marketed formulation released (44.8%) of the drug after 8 hrs. The in vitro Miconazole nitrate release data were fitted to Korsmeyerpeppa's release model. The formulation exhibited non-fickian transport with zero order kinetics. Formulae G1, G8 and G10, that showed both small droplet size and highest extent of drug release, were microbiologically evaluated against Candida albicans (C. albicans) using agar cup diffusion method. The selected formulae showed superior antimycotic activity compared to the commercially available formulation