Preparation and characterization of PEGylated liposomal Doxorubicin targeted with leptin-derived peptide and evaluation of their anti-tumor effects, in vitro and in vivo in mice bearing C26 colon carcinoma

Shahraki, Naghmeh; Mehrabian, Amin; Amiri-Darban, Shahrazad; Moosavian, Seyedeh Alia; Jaafari, Mahmoud Reza

doi:10.1016/j.colsurfb.2021.111589

Cited by 29 publications

(16 citation statements)

References 72 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…PEGylated liposomal doxorubicin decorated with a leptin-derived peptide (Lp31) showed improved uptake by and cytotoxicity against C26 cells. The results of animal experiments revealed the suppression of tumor growth, consistent with the increased doxorubicin concentration in tumor tissue [71]. A similar outcome was published by another group using leptin-derived peptide (LP16, 91-110 of leptin) to reduce tumor growth in a C26 colon carcinoma tumor-bearing mouse model [72].…”

Section: Leptin and Colorectal Cancersupporting

confidence: 83%

Leptin and Cancer: Updated Functional Roles in Carcinogenesis, Therapeutic Niches, and Developments

Lin

Hsiao

2021

IJMS

View full text Add to dashboard Cite

Leptin is an obesity-associated adipokine that is known to regulate energy metabolism and reproduction and to control appetite via the leptin receptor. Recent work has identified specific cell types other than adipocytes that harbor leptin and leptin receptor expression, particularly in cancers and tumor microenvironments, and characterized the role of this signaling axis in cancer progression. Furthermore, the prognostic significance of leptin in various types of cancer and the ability to noninvasively detect leptin levels in serum samples have attracted attention for potential clinical applications. Emerging findings have demonstrated the direct and indirect biological effects of leptin in regulating cancer proliferation, metastasis, angiogenesis and chemoresistance, warranting the exploration of the underlying molecular mechanisms to develop a novel therapeutic strategy. In this review article, we summarize and integrate transcriptome and clinical data from cancer patients together with the recent findings related to the leptin signaling axis in the aforementioned malignant phenotypes. In addition, a comprehensive analysis of leptin and leptin receptor distribution in a pancancer panel and in individual cell types of specific organs at the single-cell level is presented, identifying those sites that are prone to leptin-mediated tumorigenesis. Our results shed light on the role of leptin in cancer and provide guidance and potential directions for further research for scientists in this field.

show abstract

Section: Leptin and Colorectal Cancersupporting

confidence: 83%

Leptin and Cancer: Updated Functional Roles in Carcinogenesis, Therapeutic Niches, and Developments

Lin

Hsiao

2021

IJMS

View full text Add to dashboard Cite

show abstract

“…In addition, leptin may play an important role in the relationship between obesity and colorectal cancer [ 29 ]. Recently, several studies have been conducted to study the efficacy of leptin with some anticancer drugs such as doxorubicin [ 30 ], which treat a wide range of cancers [ 31 ].…”

Section: Resultsmentioning

confidence: 99%

Leptin hormone and its effectiveness in reproduction, metabolism, immunity, diabetes, hopes and ambitions

Al-Hussaniy¹,

Albu-Rghaif²,

Naji³

2021

JMedLife

View full text Add to dashboard Cite

Leptin is a hormone derived from adipose tissue and the small intestine, mainly in enterocytes; it helps regulate the energy balance by suppressing hunger, resulting in decreased fat mass in adipocytes. Leptin has specific receptors in the ventromedial and arcuate nuclei and other parts of the hypothalamus and the feeding center in the ventral tegmental area. It also plays a role in regulatory aspects other than fat cells, such as obesity, which is linked to a loss of sensitivity of leptin receptors, resulting in an inability to produce satiety and an increase in food intake. Moreover, leptin plays a part in lactation, bone density, the immune system, diabetes treatments, and hypertriglyceridemia. The latest studies in leptin suggest that an analog of leptin may treat DM and hypertriglyceridemia. Further research should be conducted on the effectiveness of leptin on other related diseases.

show abstract

“…These long-circulating PEGylated liposomes are also called sterically stabilized or stealth liposomes. The optimal stability of the liposomal formulations can retain the entrapped drug in circulation for a long time, reach the target sites, and exert its cytotoxic activities in cancer cells [23][24][25].…”

Section: Introductionmentioning

confidence: 99%

Safety, Stability, and Therapeutic Efficacy of Long-Circulating TQ-Incorporated Liposomes: Implication in the Treatment of Lung Cancer

et al. 2022

View full text Add to dashboard Cite

Thymoquinone (TQ), which is one of the main bioactive constituents of Nigella sativa seeds, has demonstrated its potential against various cancer models. The poor solubility of TQ in aqueous solution limits its uses in clinical application. The present study aimed to develop a novel formulation of TQ to increase its bioavailability and therapeutic potential with minimal toxicity. Polyethylene glycol (PEG)-coated DSPC/cholesterol comprising TQ liposomes (PEG-Lip-TQ) were prepared and characterized on various aspects. A computational investigation using molecular docking was used to assess the possible binding interactions of TQ with 12 prospective anticancer drug targets. The in vitro anticancer activity was assessed in A549 and H460 lung cancer cells in a time- and dose-dependent manner, while the oral acute toxicity assay was evaluated in silico as well as in vivo in mice. TQ docked to the Hsp90 target had the lowest binding energy of −6.05 kcal/mol, whereas caspase 3 was recognized as the least likely target for TQ with a binding energy of −1.19 kcal/mol. The results showed 96% EE with 120 nm size, and −10.85 mv, ζ-potential of PEG-Lip-TQ, respectively. The cell cytotoxicity data demonstrated high sensitivity of PEG-Lip-TQ and a several fold decrease in the IC50 while comparing free TQ. The cell cycle analysis showed changes in the distribution of cells with doses. The in vivo data revealed an ~9-fold increase in the LD50 of PEG-Lip-TQ on free TQ as an estimated 775 and 89.5 mg/kg b.w, respectively. This study indicates that the pharmacological and efficacy profile of PEG-lip-TQ is superior to free TQ, which will pave the way for an exploration of the effect of TQ formulation in the treatment of lung cancer in clinical settings.

show abstract

Preparation and characterization of PEGylated liposomal Doxorubicin targeted with leptin-derived peptide and evaluation of their anti-tumor effects, in vitro and in vivo in mice bearing C26 colon carcinoma

Cited by 29 publications

References 72 publications

Leptin and Cancer: Updated Functional Roles in Carcinogenesis, Therapeutic Niches, and Developments

Leptin and Cancer: Updated Functional Roles in Carcinogenesis, Therapeutic Niches, and Developments

Leptin hormone and its effectiveness in reproduction, metabolism, immunity, diabetes, hopes and ambitions

Safety, Stability, and Therapeutic Efficacy of Long-Circulating TQ-Incorporated Liposomes: Implication in the Treatment of Lung Cancer

Contact Info

Product

Resources

About