[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. · 5.26 Impact Factor
[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. · 0.94 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: 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: 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: 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. 01/2010;
[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. · 2.96 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: Immune system dysfunction is responsible for various diseases like arthritis, ulcerative colitis, asthma, allergy, parasitic diseases, cancer and infectious diseases. In clinical immunology laboratory tests, which utilize a great many of the recently elucidated principles of immunology can be performed. The results are then used by practicing physicians in the diagnosis, treatment and prognosis of the clinical disorders. Further more, qualitative and quantitative analysis of immune response has led to better understanding of pathogenesis of many clinical disorders. These understanding in turn have stimulated further basic scientific research in immunology. The degree to which the patient becomes abnormally susceptible to infections by this microbial environment depends on the extent of immunosuppression. For that the immunomodulatory study of the leaves Gymnema sylvestre R.Br. (Asclepiadaceae) was carried out by in-vitro. The aqueous extract of Gymnema sylvestre leaves was investigated for immunomodulatory activity by assessing Neutrophil locomotion and chemotaxis test, phagocytosis of killed Candida albicans and Nitroblue tetrazolium test. The extract was given at dose of 25mg/ml, 50 mg/ml and 100 mg/ml. Results of in-vitro immunomodulatory activity lead to the conclusion that the aqueous extract of Gymnema sylvestre showed predominantly significant activity on in-vitro human neutrophils in all parameters, which is compared to the standard.
[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.
[show abstract][hide abstract] ABSTRACT: Ophthalmic drug delivery is one of the most interesting and challenging endeavors facing the pharmaceutical scientist. The conventional ocular drug delivery systems like solutions, suspensions, and ointments show drawbacks such as increased precorneal elimination, high variability in efficiency, and blurred vision respectively. In situ-forming hydrogels are liquid upon instillation and undergo phase transition in the ocular cul-de-sac to form visco-elastic gel and this provides a response to environmental changes. In the past few years, an impressive number of novel temperature, pH, and ion induced in situ-forming systems have been reported for sustain ophthalmic drug delivery. Each system has its own advantages and drawbacks. The choice of a particular hydrogel depends on its intrinsic properties and envisaged therapeutic use. This review includes various temperature, pH, and ion induced in situ-forming polymeric systems used to achieve prolonged contact time of drugs with the cornea and increase their bioavailability.
Journal of Controlled Release 10/2007; 122(2):119-34. · 7.63 Impact Factor
[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.