Formulation and pharmacokinetic evaluation of hard gelatin capsule encapsulating lyophilized Vasa Swaras for improved stability and oral bioavailability of vasicine (original) (raw)
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In this present study Aspirin loaded gelatine nanoparticles were prepared by desolvation technique using acetone as desolvating agent. In the treatment of Ankylosing spondylitis and arthritis the dose of aspirin required is 3 g/ day in divided doses. As there are more chances of missing the dose of drug it is better to formulate sustained release dosage forms for better administration. Two methodologies were followed in the addition of desolvating agent to the aqueous solution of gelatine. First one was the continuous addition method and second one was the Intermittent addition method. Comparative study was performed to determine the best method for the preparation of gelatine nanoparticles. Two formulations were prepared by continuous and intermittent addition of acetone as desolvating agent to the aqueous solution of gelatine. Comparative study was made between these two Formulations for particle size, Mean particle diameter, Product yield, Drug content, Electrophoretic mobility, Zetapotential, Entrapment efficiency, Loading capacity. In vitro drug release studies were performed to determine the sustained release effect of these two gelatine Formulations. On comparison Intermittent addition method was showing Promising results. The particle size was found to be 725.3 nm. Drug content (90 %), was found to be satisfactory. The Formulation was found to be more stable with Electrophoretic mobility, Zetapotential value of-1.645,-21.3 respectively. In a time period of 8.5 hrs, 60.9 % of the drug has been released from this Formulations. On comparison the drug release was slightly more in the Formulation 2 prepared by intermittent addition method. From the results it was concluded that Intermittent addition method can be considered to be the best method for the preparation of gelatine nanoparticles. INTRODUCTION Throughout the world, continuous efforts are in progress for developing improved, optimized and advanced drug delivery system. In the recent years, for the formulation of efficacious drugs, there has been tremendous growth of research in the field of nanoscience and nanotechnology. (Robinson, 2005). The reason why these nanoparticles are attractive for the medical applications is based on the unique features like higher surface to mass ratio which provides tremendous driving force for diffusion, their quantum properties and larger surface area promoting their ability to bind, adsorb and carry drugs. Improved stability of therapeutic agents against various stress conditions can be achieved using biodegradable Nanoparticles, mainly those prepared using biodegradable polymers (Vyas, 2002). These are of nanoscale (subnano sized) colloidal particulates whose size ranges from 10-100 nm. The properties of materials change as their size approaches the nanoscale. They are composed of polymeric materials of either synthetic or natural origin. The drug can be either encapsulated in the polymeric matrix or can just be adsorbed onto the surface of the polymeric membrane. These have been widely used for their unique applications like targeting the drug to the specific site without being attacked by RES and also the release of the drug from the nanoformulation can be in a controlled and sustained manner (Rahimnejad, 2006). The important characteristics of ideal drug delivery like ability to target and control the drug release can be achieved by nanoparticles. And also nanoparticles composed of biodegradable polymer possess
In vivo half life of nanoencapsulated L-asparaginase
Journal of materials science. Materials in medicine, 2002
In the present study, antileukemic enzyme L-asparaginase (ASNase) was encapsulated into poly(3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) nanocapsules in order to decrease the immunogenicity and toxicity of the enzyme and to increase its in vivo half life in mice. Nanocapsules were prepared by water-in-oil-in-water approach and each phase was changed systematically. By changing the pH of the w(2) phase to the isolelectric point of L-ASNase, the encapsulation efficiency was increased from 23.7% to 28.0%. Also, modification of ASNase with PEG(2) increased the encapsulation efficiency from 23.7% to 27.9% and protected the enzyme against denaturation. Combination of the various optima enabled a substantial increase in the activity (0.074-0.429 U/mg nanocapsule). The enzyme activity in the blood due to unmodified PHBV nanocapsules dropped to 38% of its initial value 4 h after injection. When the same sample was tested for the enzyme content in the circulation by using the radio-labeled...