ABSTRACT
Primaquine (PQ) shows activity against the late hepatic stages and latent tissue forms of Plasmodium vivax and Plasmodium ovale. However, liver targeted PQ delivery may be useful to minimize the dose-limiting blood toxicities and side-effects of PQ. The prime objective of this study was the preparation of PQ loaded chitosan nanoparticles (PQ-CS-NPs) in order to enhance drug tolerance and to reduce dose frequency. The morphological analysis of the chitosan NPs displayed particle size in the range 287-686 nm, polydispersity index in the range 0.338-0.430 and zeta potential between 9.21 and 22.80 mV which indicated good stability. PQ-CS-NPs exhibited EE and LC as 64.28 ± 1.85% and 33.18 ± 0.975%, respectively. The in vitro drug release (Batch C7) was 97.80 ± 0.65% after 24 h. After intravenous injection of PQ-CS-NPs in mice, the lethal dose of the PQ significantly reduced when compared to that of free PQ solution.
Subject(s)
Chitosan/chemistry , Drug Carriers/chemistry , Nanoparticles/chemistry , Primaquine/chemistry , Primaquine/toxicity , Toxicity Tests , Animals , Drug Liberation , Drug Stability , Liver/cytology , Liver/drug effects , Liver/metabolism , Mice , Particle Size , Primaquine/metabolismABSTRACT
OBJECTIVE: The aim of present investigation is to enhance in vitro dissolution of poorly soluble drug glimepiride by preparing solid dispersions using modified gum karaya. MATERIALS AND METHODS: Solid dispersions of drug were prepared by solvent evaporation method using modified gum karaya as carrier. Four batches of solid dispersion (SD1, SD4, SD9, and SD14) and physical mixture (PM1, PM4, PM9, and PM14) were prepared and characterized by differential scanning colorimetry (DSC), Fourier transform infrared (FTIR) spectroscopy, powder X-Ray diffraction (X-RD), and scanning electron microscopy (SEM) studies. Equilibrium solubility studies were carried out in shaker incubator for 24 h and in vitro drug release was determined using USP Dissolution Apparatus-II. RESULTS: Maximum solubility and in vitro dissolution were observed with Batch SD4. No significant enhancement of dissolution characteristics were observed in the corresponding physical mixture PM4. Low viscosity with comparable swelling characteristics as compared to GK of modified form of gum karaya may lead to improvement in dissolution behavior of solid dispersion batches. Also, the conversion of crystalline form of drug to amorphous form may be a responsible factor, which was further confirmed by DSC, FTIR studies, and X-RD studies. SEM photographs of batch SD4 revealed porous nature of particle surface. CONCLUSION: Modified forms of natural carriers prove beneficial in dissolution enhancement of poorly soluble drugs and exhibited a great potential in novel drug delivery systems.
ABSTRACT
During the past decade formulation of vesicles as a tool to improve drug delivery, has created a lot of interest amongst the scientist working in the area of drug delivery systems. Vesicular system such as liposomes, niosomes, transferosomes, pharmacosomes and ethosomes provide an alternative to improve the drug delivery. Niosomes play an important role owing to their nonionic properties, in such drug delivery system. Design and development of novel drug delivery system (NDDS) has two prerequisites. First, it should deliver the drug in accordance with a predetermined rate and second it should release therapeutically effective amount of drug at the site of action. Conventional dosage forms are unable to meet these requisites. Niosomes are essentially non-ionic surfactant based multilamellar or unilamellar vesicles in which an aqueous solution of solute is entirely enclosed by a membrane resulting from the organization of surfactant macromolecules as bilayer. Niosomes are formed on hydration of non-ionic surfactant film which eventually hydrates imbibing or encapsulating the hydrating aqueous solution. The main aim of development of niosomes is to control the release of drug in a sustained way, modification of distribution profile of drug and for targeting the drug to the specific body site. This paper deals with composition, characterization/evaluation, merits, demerits and applications of niosomes.
