Development and Characterization of Pegylated Capecitabine Liposomal Formulations With Anticancer Activity Towards Colon Cancer

Abstract

Objective: Capecitabine is widely used in colorectal cancer treatment and has first-pass metabolism problem. Despite of its promising anticancer potential, capecitabine has not been used due to its poor solubility in water. The purpose of this study was to develop colon targeting capecitabine loaded stealth liposomes, which is a promising technique to avoid first-pass metabolism to achieve the desired bioavailability profile, increased water solubility and sustained release. Methods: Thin film hydration method was used to prepare capecitabine stealth liposomes. Prepared liposomes were characterized for drug release kinetics, stability studies, cell viability studies to determine the cytotoxic effect and in vivo studies in mice bearing colon carcinoma for evaluation of antitumor potential. Results: In vitro releases of liposomes were best fitted in the Higuchi matrix kinetic model with an n value from 0.868-0.964, indicating non-fickian release diffusion. Stability data indicated that liposomes were stable for at least 06 mo at 5±3 ° C. inhibiting activity was increased and with a Significant improvement in AUC, MRT and t1/2 observed as 29.65±5.08, µg h/ml for Stealth liposomes compared with the pure capecitabine and the conventional liposomes. Conclusion: Results suggested that Capecitabine-loaded stealth liposomes can be an effective delivery system for targeting colon cancer.

Formulation, Characterization and Optimization of Folic Acid-Tailored Daidzein Solid Lipid Nanoparticles for the Improved Cytotoxicity Against Colon Cancer Cells

“…Particle size, zeta potential and PDI were measured using an Anton Paar Litesizer 500(Malvern instrument, UK) at a scattering angle of 90 °C. The diluted dispersion was placed in a polystyrene cuvette with a path length of 10 mm and allowed to equilibrate for 120 seconds [22].…”

Design and Characterization of Calcipotriol Proniosomal Gel: In-vivo Exploration against Imiquimod-induced Psoriasis in Experimental Animals

“…On the basis of earlier reported literature higher concentrations of cholesterol and surfactants tween 80 and span 60 the rate drug entrapment was higher whereas at lower concentrations it was decreased. 26,27 Additionally, psoriasis is characterized by the release several cytokines such as interferon-γ, TNF-α and the number of interleukins involved in the inflammation are followed by infiltration of immune cells into the skin and finally hyperkeratosis. In-vivo antipsoriatic activity was evaluated on basis of PASI scorings along with primary dermal irritation study.…”

Formulation Development of Mucoadhesive Tablets for Treatment of Hypertension using Losartan Potassium

“…The swelling index was calculated using the equation provided. [25][26][27] In-vitro release study The purpose of this study was to employ the USP type II dissolution test apparatus to calculate the buccal tablet release rate in-vitro. Medicine in tablets is often released from just one side.…”

“…The infrared (IR) spectrum analysis suggested that no significant interaction between the drug and the excipients was detected (Figure 1). [26][27][28][29][30][31] Pre-compression Study Table 2 displays the outcomes of the pre-compression parameters. The bulk density and tapped density measurements were observed to fall within acceptable limits, suggesting that the packaging qualities necessary for compression are satisfactory across all formulations.…”