<p>Preparation, Characterization, and Pharmacokinetic Study of a Novel Long-Acting Targeted Paclitaxel Liposome with Antitumor Activity</p>

Abstract

Background: Breast cancer is the leading cause of cancer death in women. Chemotherapy to inhibit the proliferation of cancer cells is considered to be the most important therapeutic strategy. The development of long-circulating PEG and targeting liposomes is a major advance in drug delivery. However, the techniques used in liposome preparation mainly involve conventional liposomes, which have a short half-life, high concentrations in the liver and spleen reticuloendothelial system, and no active targeting. Methods: Four kinds of paclitaxel liposomes were prepared and characterized by various analytical techniques. The long-term targeting effect of liposomes was verified by fluorescence detection methods in vivo and in vitro. Pharmacokinetic and acute toxicity tests were conducted in ICR mice to evaluate the safety of different paclitaxel preparations. The antitumor activity of ES-SSL-PTX was investigated in detail using in vitro and in vivo human breast cancer MCF-7 cell models. Results: ER-targeting liposomes had a particle size of 137.93±1.22 nm and an acceptable encapsulation efficiency of 88.07±1.25%. The liposome preparation is best stored at 4°C, and is stable for up to 48 hrs. Cytotoxicity test on MCF-7 cells demonstrated the stronger cytotoxic activity of liposomes in comparison to free paclitaxel. We used the near-infrared fluorescence imaging technique to confirm that ES-SSL-PTX was effectively targeted and could quickly and specifically identify the tumor site. Pharmacokinetics and acute toxicity in vivo experiments were carried out. The results showed that ES-SSL-PTX could significantly prolong the half-life of the drug, increase its circulation time in vivo, improve its bioavailability and reduce its toxicity and side effects. ES-SSL-PTX can significantly improve the pharmacokinetic properties of paclitaxel, avoid allergic reaction of the original solvent, increase antitumor efficacy and reduce drug toxicity and side effects. Conclusion: ES-SSL-PTX has great potential for improving the treatment of breast cancer, thereby improving patient prognosis and quality of life.

In Vivo Assessment of Thermosensitive Liposomes for the Treatment of Port Wine Stains by Antifibrinolytic Site-Specific Pharmaco-Laser Therapy

“…In conclusion, none of the newly tested formulations offered additional benefits over the prime candidate formulation composed of DPPC:DSPE-PEG (96:4; F3 ) in terms of TA:lipid ratio, E eff , and C TA . The TA E eff s are low for all formulations compared to other liposomal encapsulants ( Table S3 [ 47 , 48 , 49 , 50 , 51 , 52 , 53 , 54 , 55 , 56 , 57 , 58 , 59 , 60 , 61 , 62 , 63 , 64 , 65 , 66 ]), which was expected as explained in Supplementary Section S3.1 . Further experiments therefore remained focused on the DPPC:DSPE-PEG (96:4) and DPPC:MPPC:DSPE-PEG (86:10:4) LUVETs.…”

“…The TA E eff s are low for all formulations compared to other liposomal encapsulants (Table S3 [47][48][49][50][51][52][53][54][55][56][57][58][59][60][61][62][63][64][65][66]), which was expected as explained in Supplementary Section S3.1. Further experiments therefore remained focused on the DPPC:DSPE-PEG (96:4) and DPPC:MPPC:DSPE-PEG (86:10:4) LUVETs.…”

Nanoparticle-Based Drug Delivery in Cancer Therapy and Its Role in Overcoming Drug Resistance

“…In the field of breast and prostate cancer ( Yari et al, 2019 ), the application of liposomes has been increasingly common ( Satsangi et al, 2015 ; Tang B. et al, 2020 ). Multiple paclitaxel liposomes have been demonstrated to have higher anti-tumor efficiency and improved bioavailability compared to free paclitaxel ( Han et al, 2020 ). Liposomal doxorubicin has been proven to reduce cardiotoxicity and has comparable efficacy in breast cancer ( O’Brien et al, 2004 ; Geisberg and Sawyer, 2010 ).…”

Recent Progress of Nanocarrier-Based Therapy for Solid Malignancies

“…Han et al fabricated PEG long-circulating liposomes loaded with PTX for targeting ERs in breast cancer. The liposome formulation can effectively target, quickly, and specifically identify the tumor site, and prolong drug action time [ 116 ]. Targets of breast cancer stem cells (BCSCs) include CD44 and CD133 receptor [ 168 , 169 ].…”