Phytosomes Loaded with Mitomycin C–Soybean Phosphatidylcholine Complex Developed for Drug Delivery

Abstract

A novel formulation system of phytosomes loaded with mitomycin C-soybean phosphatidylcholine (MMC-SPC) complex (MMC-loaded phytosomes) was prepared by a solvent evaporation method combined with a nanoprecipitation technique for the purpose of development of an MMC drug delivery system. The MMC-loaded phytosomes were evaluated by average particle size, zeta-potential, and residual drug-loading content as well as an in vitro drug release profile. Furthermore, in vitro stability tests and in vitro/vivo biological evaluations of the MMC-loaded phytosomes were performed. DSC, FTIR, and XRD demonstrated that MMC interacted physically with SPC within the phytosomes. DLS and ELS described a dispersion with an average particle size of 210.87 nm, a narrow size distribution (PDI 0.251), and a zeta-potential of -33.38 mV. SEM, TEM, and AFM images showed that the MMC-loaded phytosomes were spherical and intact vesicles. In vitro stability tests demonstrated that the average particle size and residual drug-loading content of the MMC-loaded phytosomes had no evident change at different storage conditions. In vitro drug release profiles indicated biphasic behavior with an initial burst release, followed by a subsequent prolonged sustained release. In vitro cytotoxicity assays with H(22) cells showed that the MMC-loaded phytosomes had remarkable cytotoxicity. In vivo antitumor effect of the MMC-loaded phytosomes also revealed a dose-dependent and superior curative inhibitory effect on tumor growth without loss of body weight compared to free MMC. Histopathological analysis of specimens taken from tumor tissues indicated that MMC-loaded phytosomes had lethal effect to hepatoma cell. These findings suggested that the MMC-loaded phytosomes can serve as a promising and effective formulation for drug delivery and cancer therapy.

Optimization, formulation, and characterization of multiflavonoids-loaded flavanosome by bulk or sequential technique

“…The phytosomes incorporated with individual flavonoids were synthesized using a conventional method adapted by Hou et al 25 with slight modification. The concentration of flavonoids loaded in phytosome/flavonosome was adjusted approximately equivalent to the content as in EA fraction.…”

“…Simultaneously, total mass of the carrier (PC) lipid matrix was obtained. Thus the % of DL was determined using the following formula: 25,27 DL% Amount of loaded flavonoids Total mass of the matrix = × 100 0 (3)…”

Lyophilized phytosomal nanocarriers as platforms for enhanced diosmin delivery: optimization and ex vivo permeation

“…Liquid phytosomes are anticipated to carry a negative charge ascribed to the SPC phosphate group in a water environment with a neutral pH value. 17 The authors suggest that a ratio of DSN:SPC (1:1) in LPN formula F1 was not optimum for complete complexation of all DSN molecules. This was manifested by the highest PS (537.5 nm) and ZP (-35.6 mV) values reflecting possible free DSN and SPC due to weak bonding.…”

“…Furthermore, lyophilization was employed in this study as a one-step preparation technique rather than a second drying step for the prepared phytosomes as was utilized in other studies. 17 DSC thermograms of lyophilized phytosomes will be discussed in detail in the DSC section (Figures 2 and 3).…”

“…Natural soyabean phosphatidylcholines (SPC) have always presented as outstanding candidates for clinical applications including biocompatibility, biodegradability, metabolic activity, and low toxicity and cytotoxicity compared to their synthetic alternatives. 17 In this context, SPC based drug delivery systems are promising. Phytosomes (herbosomes) constitute complexes between a natural product and natural phospholipids, such as soy phospholipids.…”