Liposomes Loaded with Cisplatin and Magnetic Nanoparticles: Physicochemical Characterization, Pharmacokinetics, and In-Vitro Efficacy

Abstract

With the aim improving drug delivery, liposomes have been employed as carriers for chemotherapeutics achieving promising results; their co-encapsulation with magnetic nanoparticles is evaluated in this work. The objective of this study was to examine the physicochemical characteristics, the pharmacokinetic behaviour, and the efficacy of pegylated liposomes loaded with cisplatin and magnetic nanoparticles (magnetite) (Cis-MLs). Cis-MLs were prepared by a modified reverse-phase evaporation method. To characterize their physicochemical properties, an evaluation was made of particle size, ζ-potential, phospholipid and cholesterol concentration, phase transition temperature (Tm), the encapsulation efficiency of cisplatin and magnetite, and drug release profiles. Additionally, pharmacokinetic studies were conducted on normal Wistar rats, while apoptosis and the cytotoxic effect were assessed with HeLa cells. We present a method for simultaneously encapsulating cisplatin at the core and also embedding magnetite nanoparticles on the membrane of liposomes with a mean vesicular size of 104.4 ± 11.5 nm and a ζ-potential of −40.5 ± 0.8 mV, affording a stable formulation with a safe pharmacokinetic profile. These liposomes elicited a significant effect on cell viability and triggered apoptosis in HeLa cells.

Liposomes Co-Encapsulating Cisplatin/Mifepristone Improve the Effect on Cervical Cancer: In Vitro and In Vivo Assessment

“…The amount of cisplatin encapsulated in liposomes is often very limited due to its water insolubility and low lipophilicity [ 46 , 47 ]. The entrapment efficiency of the liposomes for cisplatin in the present system of co-encapsulation was around 18%, similar to the value reported by Hirai et al and Toro-Cordova et al [ 35 , 47 ], and for mifepristone was about 25%. To our knowledge, there are no data in the literature on mifepristone-loaded liposomes.…”

“…Liposomes were prepared with the reverse-phase evaporation method, which has proven to be efficient for the encapsulation of cisplatin [ 24 , 35 ]. Saline solution originally served as the diluent owing to its reported stability [ 36 ].…”

Technetium-Radiolabeled Mannose-Functionalized Gold Nanoparticles as Nanoprobes for Sentinel Lymph Node Detection

“…It is well-known that the Dynamic Light Scattering (DLS) method gives an estimation of the hydrodynamic diameter of the particle, but it can be greatly affected by the particle shape and structure. In addition, a small portion of large contaminant or aggregated particles can greatly contribute to scattering; it is possible that the inclusion of ALA, MAN, and HYNIC attached to the surface of AuNps affects the estimation of the hydrodynamic diameter, giving information on the AuNp core, along with the coating and the layer of solvent particles attached to its surface [15]. These observations are consistent with the amount of ALA molecules chemisorbed on the surface of AuNP nanoparticles.…”

Aminated β-cyclodextrin-grafted Fe3O4-loaded gambogic acid magnetic nanoparticles: preparation, characterization, and biological evaluation

“…Fe 3 O 4 @NH 2 -b-CD@GA MNPs possessed better magnetic targeting, controlled release, low stimulation, and good pharmacokinetic behavior in vivo, including a lower CLz, longer halflife, and increased AUC, which indicate that they have a good promoting effect on enhancing drug accumulation and adsorption at the tumor site when compared with gambogic acid nanomagnetic systems, such as gambogic acid-loaded micelles based on chitosan derivatives, 42 magnetic nanoparticles of Fe 3 O 4 with gambogic acid, 43 GO-modied Fe 3 O 4 / SiO 2 nanoparticles with combined rhenium-188 and gambogic acid, 44 and gambogic acid-loaded magnetic Fe 3 O 4 nanoparticles. 45 Moreover, other nanomagnetic systems, such as pegylated liposomes loaded with cisplatin magnetic nanoparticles (Cis-MLs), 46 and folic acid-functionalized magnetic nanoparticles 47 also have great signicance.…”