Exploration of docetaxel palmitate and its solid lipid nanoparticles as a novel option for alleviating the rising concern of multi-drug resistance

Kaushik, Lokesh; Srivastava, Shubham; Panjeta, Anshul; Chaudhari, Dasharath; Ghadi, Rohan; Kuche, Kaushik; Malik, Ruchi; Preet, Simran; Jain, Sanyog; Raza, Kaisar

doi:10.1016/j.ijpharm.2020.119088

Cited by 26 publications

(13 citation statements)

References 51 publications

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“…They prepared conjugate-loaded SLN to enhance the solubility of this anticancer agent and improve pharmacokinetic parameters. Overall results indicate a decrease of IC50, an increased apoptotic index, lower affinity to Pgp-efflux (higher drug permeability), and improved pharmacokinetic and pharmacodynamic parameters for the conjugateloaded SLN than for free docetaxel (91). Another study demonstrated the benefits of modifying the superficial charge of nanoparticles.…”

Section: Improving Oral Bioavailability Of Anticancer Drugs By Slnmentioning

confidence: 86%

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Solid Lipid Nanoparticles: An Approach to Improve Oral Drug Delivery

et al. 2021

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Nanoparticles have shown overall beneficial effects in drug administration. Specifically, solid lipid nanoparticles (SLN) have emerged as an alternative to polymer-based systems. However, the oral administration of SLN, the first choice for conventional medications, has not been addressed due to the taboo surrounding the complicated transit that this delivery route entails. This review focuses on the encapsulation of drugs into SLN as a strategy for improving oral administration. Examples of applications of SLN to enhance the absorption and bioavailability of poorly-soluble drugs and protect acid-labile active molecules are discussed. This work also emphasizes the importance of developing SLN-based systems to treat health issues such as neurological diseases and cancer, and combat antibiotic resistance, three significant and increasingly common current public health problems. The review sections clarify how SLN can improve bioavailability, target therapeutic agents, and reduce side effects.

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Section: Improving Oral Bioavailability Of Anticancer Drugs By Slnmentioning

confidence: 86%

“…Recently, Kaushik et al (91) proposed a system consisting of docetaxel (BCS class IV) conjugated with a biocompatible lipid (palmitic acid). They prepared conjugate-loaded SLN to enhance the solubility of this anticancer agent and improve pharmacokinetic parameters.…”

Section: Improving Oral Bioavailability Of Anticancer Drugs By Slnmentioning

confidence: 99%

Solid Lipid Nanoparticles: An Approach to Improve Oral Drug Delivery

et al. 2021

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“…Their structure is intermediate between that of polymer nanocapsules and liposomes and similar to that of lipoproteins because of their oily core, which is surrounded by a surface-active membrane of polyethylene glycol (PEG, 660 Da). Interestingly, this surfactant can inhibit drug efflux through inhibition of P -gp as it has been reported with etoposide- or paclitaxel-loaded lipid nanoparticles in in vitro and in vivo studies [ 15 , 16 , 17 , 18 ]. This original and groundbreaking work on LNC [ 15 , 16 ] has paved the way for other works showing the efficacy of ferrocifen-loaded LNC against MDR tumors [ 19 , 20 , 21 , 22 , 23 , 24 , 25 , 26 ], especially in malignant glioma models.…”

Section: Introductionmentioning

confidence: 91%

pH-Responsive Lipid Nanocapsules: A Promising Strategy for Improved Resistant Melanoma Cell Internalization

Pautu

Lepeltier

Mellinger

et al. 2021

Cancers

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Despite significant advances in melanoma therapy, low response rates and multidrug resistance (MDR) have been described, reducing the anticancer efficacy of the administered molecules. Among the causes to explain these resistances, the decreased intratumoral pH is known to potentiate MDR and to reduce the sensitivity to anticancer molecules. Nanomedicines have been widely exploited as the carriers of MDR reversing molecules. Lipid nanocapsules (LNC) are nanoparticles that have already demonstrated their ability to improve cancer treatment. Here, LNC were modified with novel copolymers that combine N-vinylpyrrolidone (NVP) to impart stealth properties and vinyl imidazole (Vim), providing pH-responsive ability to address classical chemoresistance by improving tumor cell entry. These copolymers could be post-inserted at the LNC surface, leading to the property of going from neutral charge under physiological pH to positive charge under acidic conditions. LNC modified with polymer P5 (C18H37-P(NVP21-co-Vim15)) showed in vitro pH-responsive properties characterized by an enhanced cellular uptake under acidic conditions. Moreover, P5 surface modification led to an increased biological effect by protecting the nanocarrier from opsonization by complement activation. These data suggest that pH-sensitive LNC responds to what is expected from a promising nanocarrier to target metastatic melanoma.

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“…Since cancer cell proliferation and apoptosis are regulated by cellular signals, the inhibition of these signals is helpful for eliminating cancer [35]. It is worth adding that some other conjugated taxanes were reported recently, such as two novel conjugated derivatives of Chenodeoxycholic acid-Paclitaxel and Ursodeoxycholic acid-Paclitaxel that displayed similar or lesser anticancer activity compared to Paclitaxel [36], and Docetaxel-Palmitate-conjugated derivative [37] that offered a decreased IC50 compared to that of Docetaxel. IDD-1010 at a low concentration (10 nM) inhibited cell proliferation and arrested proliferating PC3-Luc cells in vitro at the G1-phase.…”

Section: In Vitro Drug Activitymentioning

confidence: 99%

A Novel Docetaxel-Biotin Chemical Conjugate for Prostate Cancer Treatment

Rayan

Shadafny²,

Falah

et al. 2022

Molecules

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A novel conjugate of docetaxel and biotin (designated as IDD-1010) was designed and chemically synthesized via an ester linkage at position 2’ carbon in docetaxel. The synthesized pure IDD-1010 exhibits a potent anti-cancer activity in in vitro and in vivo studies. At 10 nM, IDD-1010 has induced increased apoptosis and mitotic arrest of PC3-Luc prostate cancer cells, causing aneuploidy and cell death at higher concentrations. Toxicology studies indicate that the maximal tolerated dose (MTD) of IDD-1010 is 150 mg/kg in mice; equivalent to about 12.2 mg/kg of body weight, or to about an 850 mg dose for a patient weighing 70 kg. The MTD-treated mice exhibited weight gain similar to that of the control group, with no gross pathological signs at 14 days post-dosing. At a lower dose, IDD-1010 treatment did not lead to any significant weight loss in mice, although decreased the tumor volume stemming from injecting cancer cells into the dorsal loop of mouse prostate, and it was found to be more potent than Paclitaxel (reference drug). Similarly, IDD-1010 treatment significantly reduced tumor weight and thereby increased the percentage of mice survival as compared to reference drug-treated and control groups. To summarize, the described experiments using IDD-1010, as compared to the reference drug, strongly suggest a potential treatment utility with a wider therapeutic window for prostate cancer. Henceforth, clinical research on such a novel drug candidate would be greatly worthwhile.

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Exploration of docetaxel palmitate and its solid lipid nanoparticles as a novel option for alleviating the rising concern of multi-drug resistance

Cited by 26 publications

References 51 publications

Solid Lipid Nanoparticles: An Approach to Improve Oral Drug Delivery

Solid Lipid Nanoparticles: An Approach to Improve Oral Drug Delivery

pH-Responsive Lipid Nanocapsules: A Promising Strategy for Improved Resistant Melanoma Cell Internalization

A Novel Docetaxel-Biotin Chemical Conjugate for Prostate Cancer Treatment

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