[Show abstract][Hide abstract] ABSTRACT: Nanostructured lipid carriers (NLC) developed from mixtures of solid lipid and spatially incompatible liquid lipid by solvent diffusion method. This new type of lipid nanoparticles offers the advantage of improved drug loading capacity and release properties. In this study, Glyceryl distearate and Glyceryl behenate were chosen as solid lipid and Glyceryl triacetate used as liquid lipid. Ubidecarenone used as model drug was incorporated into the NLC. The influences of different type of solid lipid and liquid lipid concentration on physiochemical properties of the NLC were characterized. As a result, the drug encapsulation efficiencies were improved by adding the liquid lipid into the solid lipid of nanoparticles. NLC had higher encapsulation efficiency and drug release. In addition, in vivo study showed that the antioxidant activity of the Ubidecarenone (Co. Q10 NLC) was more effective than the Ubidecarenone (Coenzyme Q10) solution form on DPPH scavenging, anti-lipid peroxidation, lowers the effect of amnesia induced by scopolamine and increased bioavailability observed in Cmax, Tmax, and AUC. These results indicated that nanostructured lipid formulation of Ubiquinone (Coenzyme Q10) has more antioxidant activity than that of solution form and it can be used to reduce the oxidative stress and to increase the antioxidant enzyme activity in many neurodegenerative disorders such as Alzheimer's disease, Parkinson's disease etc.
Journal of Biomedical Nanotechnology 03/2013; 9(3):450-60. · 7.58 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: Inspite of the well-known antibacterial activity of Prulifloxacin, structural studies of this molecule are not reported. We discuss three new X-ray crystal structures of Prulifloxacin guest free form and its solvates with methyl ethyl ketone and nitromethane. The role of the solvent molecules in altering the crystal packing and hydrogen bonding is discussed. All the novel solid-state forms were characterized by PXRD, DSC and IR techniques.
[Show abstract][Hide abstract] ABSTRACT: The present study aimed to conceptualize pulsatile principles to develop a time dependent programmable pulsincap drug delivery system of 5-Fluorouracil, intended for chronotherapy in colorectal cancer. Microcapsules of 5-Fluorouracil were formulated by emulsification-solvent evaporation method using three different drug (5-Fluorouracil): polymer (Eudragit L-100 55) ratio (viz., 1:1, 1:2, & 1:3) and their physico-chemical properties were evaluated. The optimized formulation MC-2 was filled into formaldehyde treated hard gelatin capsules using different quantities (20 mg & 30 mg) of Gellan gum, Guar gum, Xanthan gum and Locust bean gum as hydrogel plugs to maintain a suitable lag period. Further modified capsules were coated with Eudragit S-100 (15%). In-vitro release studies of all the formulations showed that there was no drug release in acidic pH (0.1 N HCl) and in simulated intestinal fluid (pH 6.8 phosphate buffer). Drug release occurred in pH 7.4 upto 24 hrs in a controlled manner depending upon the quantity of hydrogel plug. All the formulations followed first order drug release kinetics and showed anomalous transport i.e., a combined mechanism of pure diffusion and Case II transport. Gamma scintigraphic studies concluded that the system released the drug in lower parts of GIT after a programmed lag time. In-vivo studies revealed that pulsincap system of formulation (F-3) showed good bioavailability compared to oral solution. Accelerated stability studies indicated that formulation F-3 was quite stable.
[Show abstract][Hide abstract] ABSTRACT: Paclitaxel (PTX) is an antineoplastic agent, commonly used to treat some leukemias, Hodgkin's lymphoma, as well as cancers of the bladder, breast, stomach, lung, ovaries, thyroid, soft tissue sarcoma, multiple myeloma, and others. However, expansion of the clinical utility of Paclitaxel has been limited by its liver and cardiac toxicity and myelosuppression. In the present study proliposome drug delivery system for Paclitaxel was developed, which will increase the efficacy and reduce the toxicity. Proliposomal drug delivery system for Paclitaxel was prepared by modified film hydration method using different ratio of two different carriers and same coating polymer with different concentrations. Formulations F1, F2 and F3, F4 were prepared by using Egg phosphatidylglycerol (EPG) and Distearoyl phosphatidylcholine (DSPC) as a carrier respectively and coating polymer PEGylated phospholipid (MPEG 2000-DSPE, Sodium salt). All the formulations were compared in terms of particle size, zeta potential, encapsulation efficiency, in vitro drug release. Optimized formulation F2 was evaluated for pharmacokinetics parameters and stability studies as per ICH guidelines. Stability studies revealed that 4 °C is the most suitable temperature for storage of proliposomal drug delivery system for Paclitaxel.
Journal of Nanopharmaceutics and Drug Delivery. 01/2013; 1(2).
[Show abstract][Hide abstract] ABSTRACT: The field of ocular drug delivery is one of the interesting and challenging endeavors facing the pharmaceutical scientist. Novel approaches for ophthalmic drug delivery need to be established to increase the ocular bioavailability by overcoming the inherent drawbacks of conventional dosage forms. In situ hydrogels are instilled as drops into the eye and undergoes a sol-to-gel transition in the cul-de-sac, improved ocular bioavailability by increasing the duration of contact with corneal tissue, thereby reducing the frequency of administration. The purpose of the present work was to develop an ophthalmic drug delivery system using three different gelling agents with different mechanisms for in situ gelation of Moxifloxacin hydrochloride, a fluoroquinolone antibiotic. polyox (a pH-sensitive gelling agent), sodium alginate (an ion-sensitive gelling agent), and poloxamer (a temperature-sensitive gelling agent) were employed for the formation of in situ hydrogel along with HPMC K4M as viscofying agent, which increases the residence time of the drug in the ocular cavity. The promising formulations MF(4), MF(5), and MF(9) were evaluated for pH, drug content, in vitro gelation, in vitro drug release, in vivo drug release, ocular irritation, and stability. Percent drug content of 98.2, 98.76, and 99.43%; viscosity of 15.724 × 100, 16.108 × 100, and 15.213 × 100 cP at 20 rpm, cumulative percent release of 75.364, 74.081, and 71.752%, and C (max) of 1,164.16, 1,187.09, and 1,220.58 ng/ml was observed for formulation MF(4), MF(5), and MF(9), respectively. The developed formulations were therapeutically efficacious, stable, and non-irritant and provided sustained release of the drug over 8 h.
European Journal of Drug Metabolism and Pharmacokinetics 10/2011; 37(2):117-23. · 1.31 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: Pulmonary drug delivery is a developing technology in which medication is inhaled through the lungs and enters the bloodstream through the alveolar epithelium. Pulmonary drug delivery provides a noninvasive, alternative method to subcutaneous injection, and also intravenous injection. The delivery device plays a major role in the efficiency of pulmonary delivery, and great strides have been made in the development of new devices in recent years. The devices most commonly used for respiratory delivery, including nebulizers, metered-dose inhalers, and dry powder inhalers, can all be adapted for use with protein/peptide drugs. The choice of device will depend on the drug, the formulation, the site of action, and the pathophysiology of the lungs. While a great deal of recent research has focused on the development of novel devices, attention must now be paid to the formulation of these macromolecular drugs. The emphasis in this review will be on targeting of drugs by inhalation using carriers (such as liposomes, microspheres, microparticles, and nanoparticles) and ligands.
PDA journal of pharmaceutical science and technology / PDA. 09/2011; 65(5):513-34.
[Show abstract][Hide abstract] ABSTRACT: Objective: To prepare and characterize Albumin microspheres of hydralazine hydrochloride for the treatment of hypertension. Methods: Albumin microspheres of antihypertensive drug hydralazine hydrochloride were prepared by emulsion cross-linking method by using glutaraldehyde as cross-linking agent. Drug and polymer compatibility was determined by Fourier-Transform Infrared spectroscopy. To determine the effect of polymer concentration and amount of glutaraldehyde, formulations were characterized for their entrapment efficiency, particle size, surface morphology and release behavior. In vivo study was carried out on hypertensive wistar rats. Key findings: Maximum percentage entrapment efficiency (%EE) was found to be 68.20±1.03 %. Laser particle size analyzer confirmed mean particle size in the range of 31.7 to 39.6µm. In vitro drug release studies showed a biphasic release pattern for all formulations with an initial burst effect followed by slow release for almost 24 hrs. Conclusion: In vivo study to determine antihypertensive effect of selected formulation strongly correlates with in vitro drug release behavior. The release behavior was significantly regulated by polymer concentration and volume of glutaraldehyde. The study revealed that hydralazine hydrochloride loaded albumin microspheres exhibited prolonged reduction of systolic and diastolic arterial pressure compared to hydralazine hydrochloride solution.
[Show abstract][Hide abstract] ABSTRACT: Lipid-based formulations encompass a diverse group of formulations with very different physical appearance, ranging from simple triglyceride vehicles to more sophisticated formulations such as self-emulsifying drug delivery systems (SEDDS). Lipid-based drug delivery systems may contain a broad range of oils, surfactants, and co-solvents. They represent one of the most popular approaches to overcome the absorption barriers and to improve the bioavailability of poorly water-soluble drugs. Diversity and versatility of pharmaceutical grade lipid excipients and drug formulations as well as their compatibility with liquid, semi-solid and solid dosage forms make lipid systems most complex. Digestion of triglyceride lipids, physicochemical characteristics and solubilisation of lipid digestion products as well as intestinal permeability are some of the variable parameters of such formulations. Furthermore, among the factors affecting the bioavailability of the drug from lipid-based formulations are the digestion of lipid, the mean emulsion droplet diameter, the lipophilicity of the drug and the type of lipids. The solubility of the Active Pharmaceutical Ingredient in the Lipid System, the desorption/sorption isotherm and the digestibility of lipid vehicle are important issues to be considered for formulations of isotropic lipid formulations. This review also describes the fate of lipid formulations in the gut and the factors influencing the bioavailability from lipid-based formulations. Novel formulation systems and currently marketed products conclude this review.
[Show abstract][Hide abstract] ABSTRACT: Oral route of administration have wide acceptance up to 50-60% to total drug forms. Fast disintegrating drug delivery system has number of advantage such as faster onset of action, attractive elegance, ease of administration. In this study, an attempt has been made to study direct compression method, for formulation of fast disintegrating tablets of Isoniazid and Rifampicin, an anti- tubercular drug in view of enhancing bioavailability. These formulations have sufficient hardness and can be manufactured by commonly used equipment. Prior to formulation the pre-compression parameters were characterized for flow properties and prepared formulations were evaluated for physico-chemical parameters, X-ray powder crystallography, SEM and in-vivo bioavailability. All four formulations possessed good disintegration properties with total disintegration time of 25 to 40 seconds. The effects of different superdisintegrants and process variables on drug release profile and disintegration property were evaluated and results revealed the better drug release with different superdisintegrants such as Ac-di sol and Polyplastadone XL. All formulations are rapidly disintegrated in oral cavity as well as all formulations possess good anti-tubercular properties. SEM Showed the mechanical strength of the formulations affected the morphological changes after compression. Hence, it is evident from this study that fast dispersible tablets could be a promising delivery system for Isoniazid, Rifampicin and their combination with good mouth feel and improved drug availability with better patient compliance.
International Journal of Drug Delivery. 01/2011; 2(4).
[Show abstract][Hide abstract] ABSTRACT: Purpose: To investigate the production of antibiotic from actinomycetes isolated from soil and evaluate its antimicrobial activities. Methods: In a medium formulation study, A-4 and A-4 actinomycete mutant strains (out of the six strains selected from the nine actinomycetes that were screened) were evaluated for maximum antibiotic production using various carbon and nitrogen sources. Zone of inhibition and packed cell volume were the parameters used for the evaluation. Various fermentation conditions such as pH, temperature and dissolved oxygen were also optimized for maximal production of antibiotic from both A-4 and A-4 mutant. Results: Some actinomycetes strains showed promising antimicrobial activity against different strains of bacteria and fungi. Out of the six strains selected, one strain, designated A-4, showed maximum antimicrobial property against Gram positive and Gram negative strains as well as against various fungi. Conclusion: Findings from this investigation reveal that strain A-4 and A-4 mutant strains, in that order, exhibited superior antimicrobial activities to other soil isolates of actinomycetes.
Tropical Journal of Pharmaceutical Research. 09/2010; 9(4).
[Show abstract][Hide abstract] ABSTRACT: Purpose: To isolate and characterize antibiotic producing actinomycetes from soil samples in Belgaum, Karnataka, India. Methods: Crowded plate technique was used for the isolation of actinomycetes in media such as soybean - casein digest medium and actinomycetes isolation agar. The morphological and cultural characterization of one of the selected strains, designated A-4, was performed as per International Streptomycete Project (ISP). Results: Morphological and cultural studies showed that A-4 belonged to the Actinomycete genus. The morphological and cultural characteristics of the A-4 mutant showed cellular and aerial growth as well as soluble pigment formation in various ISP media. Conclusion: Findings from this investigation revealed that the selected strain, A-4, is an actinomycete.
Tropical Journal of Pharmaceutical Research (ISSN: 1596-5996) Vol 9 Num 3. 07/2010;
[Show abstract][Hide abstract] ABSTRACT: Purpose: Two critical factors that govern the stability of pharmaceutical formulations in the tropics are humidity and temperature. This study was carried out to investigate the effect of moisture sorption at two different storage conditions on Cefaclor dry powder for oral suspension and predict the effect of moisture interaction on the reconstituted formulations Method: Cefaclor dry powder for suspension formulation was taken as a model formulation for this study. Different formulations were manufactured and placed in twelve amber coloured glass bottles for each test condition. One set of bottles was sealed by heat induction technique under vacuum to ensure the integrity of the seal while the other set was without a seal but had a child-resistant cap. Both types of bottles were stored in humidity chambers at 30°C/65%RH or 40°C/75%RH. Weight changes were monitored on a dynamic moisture balance over a period of 3 months. Results: The results were recorded in terms of moisture content, colour, and excipient interaction and their effect on product appearance. The data were analyzed using Students t-test and one way analysis of variance (ANOVA), and differences were considered statistically significant at P < 0.05. Conclusions: The study revealed that the product with enhanced packaging and also contained non-water soluble colourants were more protected against the deleterious effects of moisture and temperature. The findings provide an insight into a possible approach for formulating moisture-sensitive pharmaceutical products, especially dry powder preparations for use in the tropics.
Tropical Journal of Pharmaceutical Research (ISSN: 1596-5996) Vol 9 Num 1. 03/2010;
[Show abstract][Hide abstract] ABSTRACT: The present study was designed to evaluate targeting efficiency of carboplatin anticancer drug. Drug was encapsulated in natural biodegradable polymer sodium alginate. The nanoparticles were prepared by the ion gelification technique and evaluated for encapsulation efficiency, loading capacity, in vitro release pattern and targeting efficiency. Drug encapsulation efficiency was about 52.24-68.70% for different formulations. In vitro release profile showed duration of drug release was also increased (more than 12 h) by nanoparticulate formulation as compared to pure drug (up to 3 h). The formulations were parenterally administered to laca mice and the drug was detected in body organs like liver, lungs and spleen. In case of free drug, less amount of drug was found in liver, lungs and spleen as compared to drug encapsulated nanoparticles. Thus sodium alginate nanoparticles can be used for targeting carboplatin and it can be a promising tool in the delivery of anticancer drugs.
International Journal of Pharmaceutics 10/2009; 385(1-2):176-80. · 3.99 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: Dendrimers are new class of polymeric materials. It is generally described as a macromolecule, which is characterized by its extensively branched 3D structure that provides a high degree of surface functionality and versatility. The unique properties associated with these dendrimers such as uniform size, high degree of branching, water solubility, multivalency, well-defined molecular weight and available internal cavities make them attractive for biological and drug-delivery applications. Commercialization of dendrimers is now forthcoming. The present review briefly describes about dendrimer synthesis strategies, types of dendrimers with different functionalities, properties which having crucial importance and their potential applications.
European journal of pharmaceutical sciences: official journal of the European Federation for Pharmaceutical Sciences 08/2009; 38(3):185-96. · 2.61 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: Some new 2-Amino substituted- benzothiazole (A1-7) were synthesized by treating with KSCN in presence of glacial acetic acid and with different Substituted aniline. Structures of the synthesized compounds were established on the basis of Melting Point, TLC, and IR spectral data. The anti microbial activity of the synthesized compounds was evaluated by disc diffusion method.
[Show abstract][Hide abstract] ABSTRACT: The alcoholic extract of Gymnema sylvestre leaves was investigated for evaluation of Wound healing properties in rats at a dose 200 mg/kg. Results of in-vivo activity lead to the conclusion that the alcoholic extract of Gymnema sylvestre showed significant wound healing properties by excision, incision and dead space granuloma models.
[Show abstract][Hide abstract] ABSTRACT: Some new 2-Amino substituted- benzothiazole (A1-7) were synthesized by treating with KSCN in presence of glacial acetic acid and withdifferent Substituted aniline. Structures of the synthesized compounds were established on the basis of Melting Point, TLC, and IR spectral data. The anti-fungal activity of the synthesized compounds was evaluated by disc diffusion method.