The present study aimed to enhance the dissolution rate, therefore bioavailability, of famotidine (FMT) using its solid dispersions (SDs) with polyvinyl pyrrolidone (PVP)-K 30, milk powder, and inulin, both in-vitro and in-vivo. The study was also aimed to compare the effect of different amorphous polymers in enhancing the dissolution rate of FMT. The SDs were prepared with a 1:4 weight ratio by a solvent evaporation technique. Evaluation of the properties of the SDs was performed using dissolution, Fourier-transform infrared (FTIR) spectroscopy, and X-ray diffraction (XRD) studies. The SDs of FMT exhibited an enhanced dissolution rate. The FTIR spectroscopic studies showed the stability of FMT and the absence of well-defined drug excipient interaction. The XRD studies indicated the amorphous state of FMT in SDs. The drug release rate of all SDs formulation was found to be greater than the pure drug. Within one hour of dissolution studies, 99.43%, 92.5%, and 58.93% drug release were obtained, respectively, for PVP K-30, milk powder, and inulin. The first two were showing significantly higher release. SDs were also studied for bioavailability studies in-vivo in rats, which confirms that the SDs prepared by PVP K-30 and milk powder significantly enhancing the bioavailability of FMT. The maximum concentration of 15.05±2.45 μg/ml was achieved in 2 hours, and the area under the curve was found to be 33.78±7.3 μg. hour/ml. Therefore, the study results conclude that SDs of the FMT prepared by PVP K-30 successfully increases the dissolution and in-vivo bioavailability.
Keywords – Solid dispersion, Second generation solid dispersions, Famotidine, In-vivo bioavailability, amorphous polymers, dissolution enhancement, solubility enhancement.
Purpose: The objective of the present investigation was to assess the tumor-targeting potential of ligand-spacer engineered solid lipid nanoparticles (SLN) as nanoscale drug delivery units for site-specific delivery of a model anticancer agent, paclitaxel (PTX). SLNs were engineered by direct and indirect conjugation of folic acid (FA) through different types of polyethylene glycols (PEGs) (MW: 1000, 4000) as spacers.
Methods: The synthesized nanoconjugates (SLNFA, SLN1FA, and SLN4FA) were characterized by Fourier transform infrared spectroscopy, nuclear magnetic resonance, and transmission electron microscopic studies. Nanoconjugates were evaluated for entrapment, in vitro drug release (under various pH conditions) and hemolytic studies. Cell uptake and cytotoxicity studies were performed on human malignant cell lines (MCF-7) using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay.
Results: This study explored the effect of PEG spacer length on the targeting potential of folate-conjugated SLN. PTX entrapment and in vitro drug release from nanoconjugates augmented, and hemolytic toxicity of nanoconjugates slashed with the molecular weight of PEGs. Further, nanoconjugates with PEG 4000 displayed highest tumor-targeting potential as compared to other spacer conjugated nanoconjugates due to optimized steric hindrance and receptor mediated endocytosis among other PEGs.
Conclusion: Engineering of the dendritic surface with targeting ligand such as FA can enhance the site-specific anticancer drug delivery. PEGylation of SLN can improve the circulation time of SLN in the body. This is a debut study reporting FA conjugation to the surface through four PEGs as spacer and optimized the spacer chain length for effective cancer targeting through SLN. This report as a whole is believed to shed new light on the role of spacer chain length in targeting potential of folate-anchored SLN.
Microemulsions improve the transdermal delivery of several drugs over conventional topical preparations such as emulsions and gels: enhanced drug solubilization, increased skin flux, and decreased diffusion coefficient. Microemulsion-based systems find significant improvement in the topical delivery of antifungals. We believe that drug-loaded microemulsion will show better antifungal activity by better penetration into the skin and fungal cells. Antifungal agents are mostly lipophilic and easily formulated in topical vehicles. Microemulsions were prepared by the phase titration method. Formulations of the same drug and Excipient ratio and different concentrations were optimized with selected parameters like pseudo ternary phase diagram, particle analysis size, zeta potential validation, entrapment efficiency, and drug release studies performed by dialysis bag diffusion techniques at a temperature (37ºC). The study continued for 24 hours. The maximum amount of drug Holoptelea integrifolia release is 90% within 8hr. The study was monitored at 37ºC. Successfully done preparation, characterization, and drug release study of Microemulsion drug loaded.
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