Flurbiprofen-nicotinamide solid dispersions were prepared by the fusion method. The solid dispersions were evaluated for dissolution rate. The drug-carrier interaction in the liquid and solid states were studied by using phase solubility analysis, phase diagram, X-ray diffraction (XRD), and differential scanning calorimentry (DSC). Solid dispersions gave fast and rapid dissolution of flurbiprofen compared with the pure drug and the physical mixture. Phase diagram and DSC indicated that flurbiprofen and nicotinamide form a eutectic mixture. The aqueous solubility of flurbiprofen was enhanced in the presence of nicotinamide.
The use of electrospun nanofibers to enhance dissolution of poorly soluble drugs could be a novel strategy in future for pharmaceutical applications. In the present work electrospun nanofibers were prepared as a novel system for enhancing the delivery of piroxicam, a non-steroidal anti-inflammatory drug (NSAID). These nanofibers were prepared from polyvinyl pyrrolidone (PVP) (pharmaceutical grade), a biodegradable polymer, to obtain a solution with drug:polymer ratio of 1:4. The release rate of the piroxicam nanofibers was studied in simulated gastric fluid. Fourier transform infrared (FTIR) and scanning electron microscopy (SEM) are used to evaluate the chemical and physical nature. The results showed that the release rates were twice increased in comparison with the pure drug. However, the blend of drug and polymer could be varied to optimize the release rates depending upon the need and formulation
Labetalol is an adrenergic receptor blocking agent used in the treatment of hypertension and characterized by high solubility and high permeability which corresponds to BCS class I drug. Plasma half life ranges from 6 & bioavailability is 25%. Ethyl cellulose was used as a rate controlling polymer. Effects of addition of ethyl cellulose on in vitro dissolution were studied. Nanoparticles were formulated using different polymer ratios. In vitro drug release was carried out by using USP Type II at 50 rpm in 900 ml of acidic dissolution medium (pH 1.2) for 2 hours, followed by 900 ml alkaline dissolution medium (pH7.4) for 12 hours. Mean dissolution time is used to characterize drug release rate from a dosage form. Several kinetic models were applied to the dissolution profiles to determine the drug release kinetics. Excipients are selected by FTIR studies. Finally the nanoparticles were evaluated for various characteristics like encapsulation efficiency, percentage yield, partial size and the In vitro release for 12 hrs. The nanoparticles were found to be discrete, spherical, and free-flowing. The nanoparticles were uniform in size, and the microencapsulation efficiency was in the range of 52.5-81.7%. The surface morphology of prepared Labetalol nanoparticles was observed under scanning electron Microscopy. Nanoparticles had good spherical geometry. The stability study was performed at 40ºC ± 2ºC and 75 ± 5% RH for 6 months. Keywords: Nanoparticles; Labetalol, Hypertension, Ethyl Cellulose, Dissolution, entrapment efficiency.
The aim of present study was to formulate and evaluate nanoparticles of carvedilol by using different hydrophilic polymers. Carvedilol was selected as a suitable drug for gastro- retentive nanoparticles due to its short half life, low bioavailability, high frequency of administration, and narrow absorption window in stomach and upper part of GIT. The nano-precipitation method was used to prepare nanoparticles so as to avoid both chlorinated solvents and surfactants to prevent their toxic effect on the body. Nanoparticles of carvedilol were prepared by using hydrophilic polymers such as HPMC K100M, chitosan, and gelatin. The prepared formulations were then characterized for particle size, polydispersity index, zeta potential, loading efficiency, encapsulation efficiency and drug-excipient compatibility. The prepared nanoparticulate formulations of carvedilol with different polymers in 1:1 ratio have shown particle size in the range of 250.12-743.07 nm, polydispersity index (PDI) in the range of 0.681-1.0, zeta potential in the range of -14.2 to +33.2 mV, loading efficiency in the range of 8.74-17.54%, and entrapment efficiency in the range of 55.7%-74.2%. Nanoparticulate formulation prepared with chitosan in 1:1 ratio showed satisfactory results i.e. average particle size 312.04 nm, polydispersity index 0.681, zeta potential 33.2 mV, loading efficiency 17.54%, and entrapment efficiency 73.4%. FTIR study concluded that no major interaction occurred between the drug and polymers used in the present study. Keywords: Nanoparticles; gastro-retentive; nano-precipitation, polydispersity index, zeta potential; entrapment efficiency.
Up to 40 percent of new chemical entities discovered by the pharmaceutical industry today are poorly soluble and lipophilic compounds. The poor solubility and wettability of meloxicam leads to poor dissolution and hence the drug shows poor bioavailability. The present study is aimed at increasing the dissolution rate of the drug using the electrospinning technique. The nanofibers were prepared using the different drug:polymer ratios. The optimized formulation was characterized by fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X-ray diffraction (XRD) and the in-vitro dissolution rate studies. The meloxicam nanofibers prepared by electrospinning technique demonstrated higher drug release rate in comparison to the pure meloxicam. Moreover, in this technique the process parameters: feed rate, voltage, distance, were also optimised to obtain the maximum nanofiber yield and the satisfactory particle size.
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