Current Issue : October - December Volume : 2018 Issue Number : 4 Articles : 6 Articles
Micro- and nanoparticles have been vastly studied due to their biopharmaceutical advantages. However, these particles generally\ndisplay very weak packing and poor mechanical properties. Hereby, a new methodology is proposed to associate poorly flowing\nparticles to macrostructures targeting the improvement of flowability and redispersibility of the particles. Cecropia glaziovii-loaded\nPLGA microspheres (4.59 �± 0.04 ...
The prime objective of the present study was to check the increase in solubility and improving bioavailability of ranolazine drug. It is an antianginal and anti-ischemic drug poorly soluble in aqueous media. As the bioavailability and pharmacological response of the drug is greatly influenced by solubility. Present study investigates the effect of nanocrystals of ranolazine on solubility and to increase in bioavailability. Nanocrystals of the ranolazine were prepared by using antisolvent precipitation technique using polymer like microcrystalline cellulose (MCC), the prepared formulations were characterized by fourier transform infrared spectroscopy, x-ray diffraction study and scanning electron microscopy. Solubility study was performed to check the enhanced properties of nanocrystals of ranolazine. It was observed that, ranolazine nanocrystals exhibited significantly faster solubility compared with conventional from of a drug. The optimized batch was NC7 and ratio of ranolazine drug nanocrystals found to be 1:1 at 1500 rpm. It was found that, formulation of nanocrystals of ranolazine show increase in drug solubility and bioavailability....
Paraffin wax is potentially useful for producing spray-congealed drug-loaded\nmicroparticles with sustained-release and taste-masking properties. To date, there is little information\nabout the effects of blending lipids with paraffin wax on the melt viscosity. In addition, drug\nparticles may not be entirely coated by the paraffin wax matrix. In this study, drug-loaded paraffin\nwax microparticles were produced by spray-congealing, and the effects of lipid additives on the\nmicroparticle production were investigated. The influence of lipid additives (stearic acid, cetyl alcohol,\nor cetyl esters) and drug (paracetamol) on the rheological properties of paraffin wax were elucidated.\nFourier transform-infrared spectroscopy was conducted to investigate the interactions between the\nblend constituents. Selected formulations were spray-congealed, and the microparticles produced\nwere characterized for their size, drug content, degree of surface drug coating, and drug release.\nThe viscosity of wax-lipid blends was found to be mostly lower than the weighted viscosity when\ninteractions occurred between the blend constituents. Molten paraffin wax exhibited Newtonian\nflow, which was transformed to plastic flow by paracetamol and pseudoplastic flow by the lipid\nadditive. The viscosity was decreased with lipid added. Compared to plain wax, wax-lipid blends\nproduced smaller spray-congealed microparticles. Drug content remained high. Degree of surface\ndrug coating and drug release were also higher. The lipid additives altered the rheological properties\nand hydrophobicity of the melt and are useful for modifying the microparticle properties....
Dysphagia is common problem among all age groups, especially for geriatric and paediatric patients. Oro-dispersible tablets (ODT) are a novel dosage form that overcome the problems of dysphagia and provides a quick onset of action. The objective of the current study was to develop and evaluate orodispersible tablets of isradipine by using sublimation technique. Orodispersible tablets of isradipine were prepared by direct compression method using different concentrations of mannitol, menthol and camphor. This technique is used to increase the porosity of the tablets in which menthol and camphor were used as subliming agents which in turn forms the porous structure on the surface of tablets after sublimation. Isradipine is an antihypertensive drug used for calcium channel blocker. It is a BCS class III drug. Hence an orally disintegrating tablet formulation of acyclovir was prepared by direct compression, which was taken as the model drug for the study. The formulated tablets were evaluated for different parameters like hardness, friability and in-vitro in-vivo disintegration time along with other physical parameters. The tablets were also evaluated for drug release for 30 minutes in 0.1 N HCl using USP Type II (Paddle Method) dissolution apparatus. The in-vitro drug release study revealed that menthol and camphor (1:1) at a concentration of 10 % (Batch–F5) of the total weight of the tablet offer fast release of isradipine within 10 minutes. These tablets also dissolved within 20-25 seconds in saliva with pleasant taste and smooth mouth feel. It was concluded that oral disintegrating isradipine tablets could be prepared by direct compression using sublimation method....
The purpose of this work was to understand effect of various process variables on the entrapment efficiency, particle size of the microspheres. Microspheres were prepared by emulsion cross linking method using different drug polymer ratios (formulation F1 to F6), stirring speed and concentration of emulsifying agent. Glutaraldehyde in toluene was used for cross linking agent. The mean particle size of the microspheres significantly increased with increasing gelatin ratio and was in the range 1.69±2.14 μm to 15.11±2.15 μm. The drug entrapment of the microspheres increased initially from 56.94±3.21 % to 80.87±2.93% with the increase in the drug polymer ratio from 1:1 to 1:4, the highest entrapment efficiency was found in F4 formulation. Then it decrease 76.00±1.71 and 68.91±2.14 for 1:5 and 1:6 respectively. Stirring rate increased from 500 rpm-1500 rpm, the mean particle size of the microspheres was decreased from 12.86±1.60 μm to 3.19±1.96 μm significantly and the entrapment efficiency was decreased from 80.94±3.21 % to 72.19±1.36 %. The stirring speed has negative effect on drug entrapment efficiency. As the concentration of the emulsifying agent (Span 80) was increased from 1% to 3% w/v, the particle size of the microspheres was decreased from 9.26±1.30 μm to 4.77±1.51 μm. Increase in concentration of emulsifying agent (Span 80) decrease the encapsulation efficiency from 80.94±1.02 to 78.19±1.68 of microspheres. The higher drug to polymer ratio inversely proportional to particle size, drug entrapment efficiency and directly proportional to release rate. Whereas stirring rate of emulsion system are inversely proportional to particle size and drug entrapment efficiency and high concentration of emulsifier decrease the particle size and increase the drug entrapment efficiency of microspheres....
Cyanine dyes are promising candidates in biomedical applications. Although various\ndelivery systems have been developed to enhance their properties, their dendrimer-based delivery\nsystems are seldom investigated. Herein, amine-terminated generation 5 poly(amidoamine)\n(G5.NH2) dendrimers and new indocyanine green (IR820) dyes were chosen as models to study\nthe loading ability of dendrimers for cyanine dynes. G5.NH2 dendrimers were pre-modified with\narginine-glycine-aspartic (RGD) peptides, poly(ethylene glycol) chains, and acetyl groups to be\nendowed with cancer cell specificity and biocompatibility. The formed Ac-PR dendrimers were used\nto load IR820, followed by thorough characterization. The loaded number of IR820 was estimated to\nbe 6.7 per dendrimer. The stability of IR820 was improved through dendrimer loading, which was\nproved by their UV-vis spectra under different kinds of storage conditions. In addition, the formed\nAc-PR dendrimers can retain the loaded IR820 effectively. Their cytocompatibility was desirable under\nthe studied conditions. Their cellular uptake behaviors were demonstrated to be enhanced by RGD\nmodification, showing concentration-, co-incubation time-, and �±v�²3 integrin receptor-dependent\nproperties, displaying a cytoplasm-location. The findings from this work demonstrated the versatile\nloading and delivery capacity of dendrimers for near-infrared (NIR) dyes, providing fundamental\ndata for the development of dendrimer/NIR dye systems for biomedical applications, especially for\ncancer theranostic applications....
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