Sclareol is a potent enhancer of doxorubicin: Evaluation of the free combination and co-loaded nanostructured lipid carriers against breast cancer

Borges, Gabriel Silva Marques; Silva, Juliana de Oliveira; Fernandes, Renata Salgado; Souza, Ângelo Malachias de; Cassali, Geovanni Dantas; Yoshida, María Irene; Leite, Elaine Amaral; Barros, André Luís Branco de; Ferreira, Lucas Antônio Miranda

doi:10.1016/j.lfs.2019.116678

Cited by 26 publications

(9 citation statements)

References 58 publications

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“…Through this strategy, DOX forms an ion pair with a lipophilic anion, improving its lipophilicity and the affinity for the lipid matrix. This strategy is well described in the literature and has been used in several studies that utilized different counter ions to improve the DOX lipophilicity and its affinity for different lipid-based systems [ 33 , 41 , 43 , 44 , 45 , 46 , 47 , 48 , 49 , 50 , 51 , 52 , 53 , 54 , 55 , 56 ]. In the present study, OA was used as the counter ion.…”

Section: Discussionmentioning

confidence: 99%

“…It is interesting to note that, although the encapsulation of DOX in NLC using the ion pair strategy can allow a controlled drug release at pH 7.4, it can be different in the tumor microenvironment. In other studies of our group different formulations of NLC-DOX, produced with different counter ions, showed that NLC-DOX is more efficient in reaching toxic levels of DOX in tumor cells, when compared to free DOX [ 33 , 56 ]. This occurs because, in the acid environment of the tumor area [ 85 ], there is an increase in the protonation of the COOH group of OA and a consequent decrease in the ion pair interaction, facilitating the release of DOX in the tumor microenvironment [ 71 ].…”

Section: Discussionmentioning

confidence: 99%

“…Through this strategy, DOX forms an ion pair with a lipophilic anion, improving its lipophilicity and the affinity for the lipid matrix. This strategy has improved the efficacy of DOX, as well as reduced its toxicity in different lipid-based systems [ 33 , 41 , 43 , 44 , 45 , 46 , 47 , 48 , 49 , 50 , 51 , 52 , 53 , 54 , 55 , 56 ].…”

Section: Introductionmentioning

confidence: 99%

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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: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Nanoencapsulated Doxorubicin Prevents Mucositis Development in Mice

et al. 2021

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“…Borges et al, have also calculated the CI for the co-encapsulation of DOX and the bicyclic diterpene alcohol sclareol in human breast cancer cells. The CI obtained for the IC 50 value was ≈0.35 [61], implying a synergistic effect with an SI value of 2.85. It can be concluded that the SI values we obtained were higher, therefore the combination of PTX and JO is more synergistic.…”

Section: Discussionmentioning

confidence: 86%

Targeted Nanoparticles Harboring Jasmine-Oil-Entrapped Paclitaxel for Elimination of Lung Cancer Cells

Engelberg

Yuexi

Assaraf

2021

IJMS

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Selectively targeted drug delivery systems are preferable chemotherapeutic platforms, as they specifically deliver the drug cargo into tumor cells, while minimizing untoward toxic effects. However, these delivery systems suffer from insufficient encapsulation efficiency (EE), encapsulation capacity (EC), and premature drug release. Herein, we coencapsulated paclitaxel (PTX) and Jasmine oil (JO) within PEG-PCL nanoparticles (NPs), with an average diameter < 50 nm, selectively targeted to non-small cell lung cancer (NSCLC) cells, via S15-aptamer (APT) decoration. JO was selected as an “adhesive” oily core to enhance PTX entrapment, as JO and PTX share similar hydrophobicity and terpenoid structure. JO markedly enhanced EE of PTX from 23% to 87.8% and EC from 35 ± 6 to 74 ± 8 µg PTX/mg PEG-PCL. JO also markedly increased the residual amount of PTX after 69 h, from 18.3% to 65%. Moreover, PTX cytotoxicity against human NSCLC A549 cells was significantly enhanced due to the co-encapsulation with JO; the IC50 value for PTX encapsulated within JO-containing APT-NPs was 20-fold lower than that for APT-NPs lacking JO. Remarkably, JO-containing APT-NPs displayed a 6-fold more potent cell-killing, relatively to the free-drug. Collectively, these findings reveal a marked synergistic contribution of JO to the cytotoxic activity of APT-NP-based systems, for targeted PTX delivery against NSCLC, which may be readily applied to various hydrophobic chemotherapeutics.

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“…In 2019, Borges et al [98] explored the codelivery of DOX and sclareol (SC), a natural diterpene, by NLCs, aiming for the treatment of breast cancer. The DOX/SC-NLC formulation was tested in vitro in MDA-MB-231 and 4T1 breast cancer cells.…”

Section: Dox and Sclareolmentioning

confidence: 99%

Antineoplastics Encapsulated in Nanostructured Lipid Carriers

et al. 2021

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Ideally, antineoplastic treatment aims to selectively eradicate cancer cells without causing systemic toxicity. A great number of antineoplastic agents (AAs) are available nowadays, with well-defined therapeutic protocols. The poor bioavailability, non-selective action, high systemic toxicity, and lack of effectiveness of most AAs have stimulated the search for novel chemotherapy protocols, including technological approaches that provide drug delivery systems (DDS) for gold standard medicines. Nanostructured lipid carriers (NLC) are DDS that contain a core of solid and lipid liquids stabilised by surfactants. NLC have high upload capacity for lipophilic drugs, such as the majority of AAs. These nanoparticles can be prepared with a diversity of biocompatible (synthetic or natural) lipid blends, administered by different routes and functionalised for targeting purposes. This review focused on the research carried out from 2000 to now, regarding NLC formulations for AAs (antimetabolites, antimitotics, alkylating agents, and antibiotics) encapsulation, with special emphasis on studies carried out in vivo. NLC systems for codelivery of AAs were also considered, as well as those for non-classical drugs and therapies (natural products and photosensitisers). NLC have emerged as powerful DDS to improve the bioavailability, targeting and efficacy of antineoplastics, while decreasing their toxic effect in the treatment of different types of cancer.

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Sclareol is a potent enhancer of doxorubicin: Evaluation of the free combination and co-loaded nanostructured lipid carriers against breast cancer

Cited by 26 publications

References 58 publications

Nanoencapsulated Doxorubicin Prevents Mucositis Development in Mice

Nanoencapsulated Doxorubicin Prevents Mucositis Development in Mice

Targeted Nanoparticles Harboring Jasmine-Oil-Entrapped Paclitaxel for Elimination of Lung Cancer Cells

Antineoplastics Encapsulated in Nanostructured Lipid Carriers

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