Development of a Method to Evaluate the Release Profile of Tamoxifen from Pegylated Hybrid Micelles

Souza, Marina Claro de; Marotta-Oliveira, Samantha S.; Rocha, Nathália Helena Souza; Eloy, Josimar O.; Marchetti, Juliana Maldonado

doi:10.1080/10826076.2015.1032418

Cited by 8 publications

(4 citation statements)

References 33 publications

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“…In vitro release studies are an essential step during drug development because not only it serves for quality control of formulations, but can also reflect the in vivo performance of the product [30]. This analysis is particularly well described for PAC, considering the publications available, reporting the sustained release of PAC from nanoparticles evaluated through the dialysis method [26,36].…”

Section: Resultsmentioning

confidence: 99%

“…In this study, samples were dispersed in 1 mL of PBS buffer, pH 7.4, and placed inside PVC tubes wrapped with 12–14 kDa MWCO (molecular weight cut-off) cellulose dialysis membranes (Fisherbrand) and connected to the dissolution shafts of the apparatus 1 (SR8 Plus, Hanson Coorporation) [30]. Samples were collected until 72 h, diluted with acetronitrile, filtered, and analyzed by the HPLC method described previously described for PAC.…”

Section: Methodsmentioning

confidence: 99%

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Co-loaded paclitaxel/rapamycin liposomes: Development, characterization and in vitro and in vivo evaluation for breast cancer therapy

Eloy

Petrilli

Topan

et al. 2016

Colloids and Surfaces B: Biointerfaces

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128

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Paclitaxel and rapamycin have been reported to act synergistically to treat breast cancer. Albeit paclitaxel is available for breast cancer treatment, the most commonly used formulation in the clinic presents side effects, limiting its use. Furthermore, both drugs present pharmacokinetics drawbacks limiting their in vivo efficacy and clinic combination. As an alternative, drug delivery systems, particularly liposomes, emerge as an option for drug combination, able to simultaneously deliver co-loaded drugs with improved therapeutic index. Therefore, the purpose of this study is to develop and characterize a co-loaded paclitaxel and rapamycin liposome and evaluate it for breast cancer efficacy both in vitro and in vivo. Results showed that a SPC/Chol/DSPE-PEG (2000) liposome was able to co-encapsulate paclitaxel and rapamycin with suitable encapsulation efficiency values, nanometric particle size, low polydispersity and neutral zeta potential. Taken together, FTIR and thermal analysis evidenced drug conversion to the more bioavailable molecular and amorphous forms, respectively, for paclitaxel and rapamycin. The pegylated liposome exhibited excellent colloidal stability and was able to retain drugs encapsulated, which were released in a slow and sustained fashion. Liposomes were more cytotoxic to 4T1 breast cancer cell line than the free drugs and drugs acted synergistically, particularly when co-loaded. Finally, in vivo therapeutic evaluation carried out in 4T1-tumor-bearing mice confirmed the in vitro results.The co-loaded paclitaxel/rapamycin pegylated liposome better controlled tumor growth compared to the solution. Therefore, we expect that the formulation developed herein might be a contribution for future studies focusing on the clinical combination of paclitaxel and rapamycin.

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Section: Resultsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Co-loaded paclitaxel/rapamycin liposomes: Development, characterization and in vitro and in vivo evaluation for breast cancer therapy

Eloy

Petrilli

Topan

et al. 2016

Colloids and Surfaces B: Biointerfaces

Self Cite

128

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“…The samples were collected in the receptor compartment in different times, from 30 min to 72 h, with replacement with fresh medium at every time. Afterwards they were diluted, filtered (0.45 µm) and analyzed by the HPLC (L-2455U, Hitachi, Japan) method [ 28 ].…”

Section: Methodsmentioning

confidence: 99%

DOPE/CHEMS-Based EGFR-Targeted Immunoliposomes for Docetaxel Delivery: Formulation Development, Physicochemical Characterization and Biological Evaluation on Prostate Cancer Cells

et al. 2023

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Docetaxel (DTX) is a non-selective antineoplastic agent with low solubility and a series of side effects. The technology of pH-sensitive and anti-epidermal growth factor receptor (anti-EGFR) immunoliposomes aims to increase the selective delivery of the drug in the acidic tumor environment to cells with EFGR overexpression. Thus, the study aimed to develop pH-sensitive liposomes based on DOPE (dioleoylphosphatidylethanolamine) and CHEMS (cholesteryl hemisuccinate), using a Box–Behnken factorial design. Furthermore, we aimed to conjugate the monoclonal antibody cetuximab onto liposomal surface, as well as to thoroughly characterize the nanosystems and evaluate them on prostate cancer cells. The liposomes prepared by hydration of the lipid film and optimized by the Box–Behnken factorial design showed a particle size of 107.2 ± 2.9 nm, a PDI of 0.213 ± 0.005, zeta potential of −21.9 ± 1.8 mV and an encapsulation efficiency of 88.65 ± 20.3%. Together, FTIR, DSC and DRX characterization demonstrated that the drug was properly encapsulated, with reduced drug crystallinity. Drug release was higher in acidic pH. The liposome conjugation with the anti-EGFR antibody cetuximab preserved the physicochemical characteristics and was successful. The liposome containing DTX reached an IC50 at a concentration of 65.74 nM in the PC3 cell line and 28.28 nM in the DU145 cell line. Immunoliposome, in turn, for PC3 cells reached an IC50 of 152.1 nM, and for the DU145 cell line, 12.60 nM, a considerable enhancement of cytotoxicity for the EGFR-positive cell line. Finally, the immunoliposome internalization was faster and greater than that of liposome in the DU145 cell line, with a higher EGFR overexpression. Thus, based on these results, it was possible to obtain a formulation with adequate characteristics of nanometric size, a high encapsulation of DTX and liposomes and particularly immunoliposomes containing DTX, which caused, as expected, a reduction in the viability of prostate cells, with high cellular internalization in EGFR overexpressing cells.

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“…Tamoxifen has a powerful anti-tumor effect on both pre and postmenopausal women as it struggles to occupy intracellular estrogen receptor sites in the target tissue and thus blocks the action of biologically active estrogens [4] . However, long-term treatment with TC causes vomiting, nausea, abdominal cramps, pulmonary embolism, ocular problems, venous thrombosis, thromboembolic disorders, and endometrial cancer [5] . Furthermore, 30-40% of women with estrogen receptor-positive breast cancer will develop metastases and die even with TC treatment [6] .…”

Section: Introductionmentioning

confidence: 99%

Potential Modulatory Effect of Sodium Butyrate on Tamoxifen Citrate-Induced Damage in the Small Intestine of Rats

Hussein

2022

Egyptian Journal of Zoology

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Tamoxifen was approved for breast cancer chemoprevention in high-risk women despite its side effects, especially on gastrointestinal tract. Therefore, this study aimed to demonstrate the therapeutic and protective properties of sodium butyrate (SB; 300 mg/kg body weight) against the small intestine injury induced by tamoxifen citrate (TC; 40 mg/kg body weight) in rats. Forty-nine male Wistar rats were randomly allotted into 5 main groups: the control group (where the rats received oral saline), SB group, TC group, SB-TC group (where SB was given before TC), and TC-SB group (where TC was given before SB). SB in TC-SB group increased the regenerative capacity of damaged intestinal tissue, decreased significantly (P<0.05) the level of intestinal malondialdehyde, and increased significantly (P<0.05) the reduced glutathione level and the activities of glutathione peroxidase, catalase, and superoxide dismutase in the intestinal tissues compared with the TC-treated group. SB also suppressed the proinflammatory cytokine response and reduced oxidative DNA damage in the intestinal tissues of the TC-SB group compared with the TC-treated group. In conclusion, this study suggested that SB reduced the harmful effects of TC on the intestinal tissues of the rats by reducing oxidative stress and decreasing the generation of proinflammatory cytokines.

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Development of a Method to Evaluate the Release Profile of Tamoxifen from Pegylated Hybrid Micelles

Cited by 8 publications

References 33 publications

Co-loaded paclitaxel/rapamycin liposomes: Development, characterization and in vitro and in vivo evaluation for breast cancer therapy

Co-loaded paclitaxel/rapamycin liposomes: Development, characterization and in vitro and in vivo evaluation for breast cancer therapy

DOPE/CHEMS-Based EGFR-Targeted Immunoliposomes for Docetaxel Delivery: Formulation Development, Physicochemical Characterization and Biological Evaluation on Prostate Cancer Cells

Potential Modulatory Effect of Sodium Butyrate on Tamoxifen Citrate-Induced Damage in the Small Intestine of Rats

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