Doxorubicin liposomes cell penetration enhancement and its potential drawbacks for the tumor targeting efficiency

Popilski, Hen; Feinshtein, Valeria; Kleiman, Sivan; Mattarei, Andrea; Garofalo, Mariangela; Salmaso, Stefano; Stepensky, David

doi:10.1016/j.ijpharm.2020.120012

Cited by 13 publications

(5 citation statements)

References 31 publications

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“…However, there is still a pressing need for fewer toxic drugs formulation and presentation. In order to circumvent the adverse effects of DOX and improve its efficacy, different drug delivery systems have been developed [ 21 , 22 , 23 , 24 , 25 , 26 , 27 , 28 , 29 , 30 ]. Among lipid-based systems, Doxil ® and Myocet ® are liposomal commercial formulations, which improved the safety profile of DOX in comparison with free DOX.…”

Section: Introductionmentioning

confidence: 99%

Nanoencapsulated Doxorubicin Prevents Mucositis Development in Mice

et al. 2021

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Doxorubicin (DOX), a chemotherapy drug successfully used in the therapy of various types of cancer, is currently associated with the mucositis development, an inflammation that can cause ulcerative lesions in the mucosa of the gastrointestinal tract, abdominal pain and secondary infections. To increase the safety of the chemotherapy, we loaded DOX into nanostructured lipid carriers (NLCs). The NLC–DOX was characterized by HPLC, DLS, NTA, Zeta potential, FTIR, DSC, TEM and cryogenic-TEM. The ability of NLC–DOX to control the DOX release was evaluated through in vitro release studies. Moreover, the effect of NLC–DOX on intestinal mucosa was compared to a free DOX solution in C57BL/6 mice. The NLC–DOX showed spherical shape, high drug encapsulation efficiency (84.8 ± 4.6%), high drug loading (55.2 ± 3.4 mg/g) and low average diameter (66.0–78.8 nm). The DSC and FTIR analyses showed high interaction between the NLC components, resulting in controlled drug release. Treatment with NLC–DOX attenuated DOX-induced mucositis in mice, improving shortening on villus height and crypt depth, decreased inflammatory parameters, preserved intestinal permeability and increased expression of tight junctions (ZO-1 and Ocludin). These results indicated that encapsulation of DOX in NLCs is viable and reduces the drug toxicity to mucosal structures.

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Section: Introductionmentioning

confidence: 99%

Nanoencapsulated Doxorubicin Prevents Mucositis Development in Mice

et al. 2021

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“…Orthotopic BxPC3 pancreatic ductal adenocarcinoma was selected in this study, and the SCGLN loaded with gemcitabine showed great tumor permeability [ 29 ]. Cell penetration enhancers (CPEs) were added to PEGylated doxorubicin liposomes (PLD) [ 284 ] to make them more effective in penetrating tumors. A MMP-2 responsive peptide-hybrid liposome (MRPL) was constructed in response to overexpressed MMP-2 in the tumor microenvironment [ 62 ].…”

Section: Application Of Other Artificially Modified Nanocarriersmentioning

confidence: 99%

Enhancing drug penetration in solid tumors via nanomedicine: Evaluation models, strategies and perspectives

Shen,

Pan,

Gong

et al. 2024

Bioactive Materials

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“…CPEs comprise a group of agents that can be linked to nanoparticles and promote their passage through the cell membrane and other cellular barriers in an ATP-dependent and independent manner [ 68 , 69 ]. Particularly, CPEs have positively charged amino acids, which facilitate their crossing of the negatively charged cell membrane [ 70 ]. CPEs can be of peptidic or non-peptidic nature.…”

Section: Modified-pegylated Liposomal Doxorubicinmentioning

confidence: 99%

“…On the other hand, the main concern with CPE-conjugated PLD is that the CPE can enhance biodistribution to other organs and lead to systematic toxicity. Nevertheless, Stepensky’s group demonstrated that despite the high accumulation of DAG-Arg4-PLD in the lung, no enhanced distribution was observed in the heart [ 70 ].…”

Section: Modified-pegylated Liposomal Doxorubicinmentioning

confidence: 99%

Recent Preclinical and Clinical Progress in Liposomal Doxorubicin

Aloss

Hamar

2023

Pharmaceutics

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Doxorubicin (DOX) is a potent anti-cancer agent that has garnered great interest in research due to its high efficacy despite dose-limiting toxicities. Several strategies have been exploited to enhance the efficacy and safety profile of DOX. Liposomes are the most established approach. Despite the improvement in safety properties of liposomal encapsulated DOX (in Doxil and Myocet), the efficacy is not superior to conventional DOX. Functionalized (targeted) liposomes present a more effective system to deliver DOX to the tumor. Moreover, encapsulation of DOX in pH-sensitive liposomes (PSLs) or thermo-sensitive liposomes (TSLs) combined with local heating has improved DOX accumulation in the tumor. Lyso-thermosensitive liposomal DOX (LTLD), MM-302, and C225-immunoliposomal(IL)-DOX have reached clinical trials. Further functionalized PEGylated liposomal DOX (PLD), TSLs, and PSLs have been developed and evaluated in preclinical models. Most of these formulations improved the anti-tumor activity compared to the currently available liposomal DOX. However, the fast clearance, the optimization of ligand density, stability, and release rate need more investigations. Therefore, we reviewed the latest approaches applied to deliver DOX more efficiently to the tumor, preserving the benefits obtained from FDA-approved liposomes.

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Doxorubicin liposomes cell penetration enhancement and its potential drawbacks for the tumor targeting efficiency

Cited by 13 publications

References 31 publications

Nanoencapsulated Doxorubicin Prevents Mucositis Development in Mice

Nanoencapsulated Doxorubicin Prevents Mucositis Development in Mice

Enhancing drug penetration in solid tumors via nanomedicine: Evaluation models, strategies and perspectives

Recent Preclinical and Clinical Progress in Liposomal Doxorubicin

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