Pteroyl-γ-l-glutamate/Pluronic® F68 modified polymeric micelles loaded with docetaxel for targeted delivery and reduced toxicity

Rarokar, Nilesh R.; Khatry, Roshani Agrawal; Yadav, Sakshi; Khedekar, Pramod B.; Ravikumar, C.R.; Telange, Darshan R.; Gurav, Shailendra

doi:10.1016/j.molliq.2022.120842

Cited by 23 publications

(7 citation statements)

References 54 publications

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“…The lowest PDI values were shown for the 1.5/1 and 3/1 Pluronic ® F68/VES-GEM micelles, as increasing the copolymer concentration may increase the solubility of the VES-GEM prodrug conjugate and contribute to a more homogeneously dispersed population, and optimal PDI values are reported for 6/1 Pluronic ® F68/VES-GEM micelles (<0.2). Regarding the Pluronic ® F127/VES-GEM micelles, varying the molar ratio resulted in micelles in the range of 100-200 nm with a slightly negative surface charge, and the same was verified for Pluronic ® F68/VES-GEM micelles (Figure 4F-H) [52]. PDI values for Pluronic ® F127/VES-GEM micelles were >0.8 for all formulations indicating the heterogeneity of the population.…”

Section: Pluronic ® /Ves-gem Conjugate Micelle Preparation and Charac...supporting

confidence: 61%

“…Regarding the Pluronic ® F127/VES-GEM micelles, varying the molar ratio resulted in micelles in the range of 100–200 nm with a slightly negative surface charge, and the same was verified for Pluronic ® F68/VES-GEM micelles ( Figure 4 F–H) [ 52 ]. PDI values for Pluronic ® F127/VES-GEM micelles were >0.8 for all formulations indicating the heterogeneity of the population.…”

Section: Resultsmentioning

confidence: 63%

“…Their hydrophilic–lipophilic balance (HLB) value is within 20–29 and the PPO chain length of Pluronic ® F127 is twice that of Pluronic ® F68 [ 48 , 49 ]. Recently, mixed Pluronic ® F68 micelles were loaded with docetaxel (20 mg/mL F68, 2% w / v ; 0.8 mg/mL docetaxel, 0.08% w / v ) [ 52 ] and curcumin (5 mg/mL F68, 0.5% w / v ; 1 mg/mL curcumin, 0.1% w / v ) [ 53 ] and Pluronic ® F127 (F127) micelles were investigated for delivery of curcumin (20 mg/mL of F127, 2% w / v ; 0.1 mg/mL, 0.01% w / v curcumin) [ 54 ], alpha-lipoic acid (20 mg/mL of F127, 2% w / v ; 10 mg/mL, 1% w / v ) [ 55 ], hypericin [ 56 ], β-escin (5 mg/mL F127, 0.5% w / v , 5 mg/mL β-escin, 0.5% w / v ) [ 57 ], boron-dipyrromethene dimer [ 58 ], lenvantinib [ 59 ], and a photosensitizer (1.11 mg/mL F127, 0.11% w / v ) [ 60 ], hence comprising biofunctional and suitable delivery systems for loading poorly water-soluble drugs with enhanced stability. Mixed Pluronic ® micelles have also been reported in the literature as a means to increase the solubility profile of poorly water-soluble drugs [ 61 , 62 ].…”

Section: Introductionmentioning

confidence: 99%

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Gemcitabine-Vitamin E Prodrug-Loaded Micelles for Pancreatic Cancer Therapy

Pereira-Silva,

Miranda-Pastoriza,

Diaz-Gomez

et al. 2024

Pharmaceutics

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Pancreatic cancer (PC) is an aggressive cancer subtype presenting unmet clinical challenges. Conventional chemotherapy, which includes antimetabolite gemcitabine (GEM), is seriously undermined by a short half-life, its lack of targeting ability, and systemic toxicity. GEM incorporation in self-assembled nanosystems is still underexplored due to GEM’s hydrophilicity which hinders efficient encapsulation. We hypothesized that vitamin E succinate–GEM prodrug (VES-GEM conjugate) combines hydrophobicity and multifunctionalities that can facilitate the development of Pluronic®F68 and Pluronic®F127 micelle-based nanocarriers, improving the therapeutic potential of GEM. Pluronic®F68/VES-GEM and Pluronic®F127/VES-GEM micelles covering a wide range of molar ratios were prepared by solvent evaporation applying different purification methods, and characterized regarding size, charge, polydispersity index, morphology, and encapsulation. Moreover, the effect of sonication and ultrasonication and the influence of a co-surfactant were explored together with drug release, stability, blood compatibility, efficacy against tumour cells, and cell uptake. The VES-GEM conjugate-loaded micelles showed acceptable size and high encapsulation efficiency (>95%) following an excipient reduction rationale. Pluronic®F127/VES-GEM micelles evidenced a superior VES-GEM release profile (cumulative release > 50%, pH = 7.4), stability, cell growth inhibition (<50% cell viability for 100 µM VES-GEM), blood compatibility, and extensive cell internalization, and therefore represent a promising approach to leveraging the efficacy and safety of GEM for PC-targeted therapies.

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Section: Pluronic ® /Ves-gem Conjugate Micelle Preparation and Charac...supporting

confidence: 61%

Section: Resultsmentioning

confidence: 63%

Section: Introductionmentioning

confidence: 99%

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Gemcitabine-Vitamin E Prodrug-Loaded Micelles for Pancreatic Cancer Therapy

Pereira-Silva,

Miranda-Pastoriza,

Diaz-Gomez

et al. 2024

Pharmaceutics

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show abstract

“…There is a wide variety of food that contains folate, and it also takes part in metabolic processes. Study reveals that most tumor cells contain folate receptors ( Rarokar et al, 2023a , Rarokar et al, 2023b , Rarokar et al, 2023c , Rarokar et al, 2023d ). Folate receptor shows more affinity towards carboxyl deuterogenic modified folic acid complex.…”

Section: Classificationmentioning

confidence: 99%

Magnetic nanosystem a tool for targeted delivery and diagnostic application: Current challenges and recent advancement

Rarokar,

Yadav,

Saoji

et al. 2024

International Journal of Pharmaceutics: X

Self Cite

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“…Pluronics are amphiphilic triblock copolymers, which are composed of hydrophilic polyethylene oxide (PEO) and hydrophobic polypropylene oxide (PPO) blocks (PEO–PPO–PEO) 14 , 15 . They are widely used in the preparation of PM due to their potential solubilizing effect, and their inhibition of P-glycoprotein (P-gp) efflux, in addition to their increased circulation time 16 .…”

Section: Introductionmentioning

confidence: 99%

An approach for an enhanced anticancer activity of ferulic acid-loaded polymeric micelles via MicroRNA-221 mediated activation of TP53INP1 in caco-2 cell line

Sweed,

Dawoud,

Aborehab

et al. 2024

Sci Rep

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Ferulic acid (FA) has powerful antioxidant and antitumor activities, but it has low bioavailability owing to its poor water solubility. Our aim is to formulate polymeric mixed micelles loaded with FA to overcome its poor solubility and investigate its potential anticancer activity via miRNA-221/TP53INP1 axis-mediated autophagy in colon cancer. A D-optimal design with three factors was used for the optimization of polymeric mixed micelles by studying the effects of each of total Pluronics mixture (mg), Pluronic P123 percentage (%w/w), and drug amount (mg) on both entrapment efficiency (EE%) and particle size. The anticancer activity of FA and Tocopheryl polyethylene glycol 1000 succinate (TPGS) mixed micelles formula (O2) was assessed by MTT and flow cytometry. O2 showed an EE% of 99.89%, a particle size of 13.86 nm, and a zeta potential of − 6.02 mv. In-vitro drug release studies showed a notable increase in the release rate of FA from O2, as compared to the free FA. The (IC50) values for FA from O2 and free FA were calculated against different cell lines showing a prominent IC50 against Caco-2 (17.1 µg/ml, 191 µg/ml respectively). Flow cytometry showed that FA caused cell cycle arrest at the G2/M phase in Caco-2. RT-PCR showed that O2 significantly increased the mRNA expression level of Bax and CASP-3 (4.72 ± 0.17, 3.67 ± 0.14), respectively when compared to free FA (2.59 ± 0.13, 2.14 ± 0.15), while miRNA 221 levels were decreased by the treatment with O2 (0.58 ± 0.02) when compared to free FA treatment (0.79 ± 0.03). The gene expression of TP53INP1 was increased by the treatment with O2 compared to FA at P < 0.0001. FA-loaded TPGS mixed micelles showed promising results for enhancing the anticancer effect of FA against colorectal cancer, probably due to its enhanced solubility. Thus, FA-loaded TPGS mixed micelles could be a potential therapeutic agent for colorectal cancer by targeting miRNA-221/TP53INP1 axis-mediated autophagy.

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Pteroyl-γ-l-glutamate/Pluronic® F68 modified polymeric micelles loaded with docetaxel for targeted delivery and reduced toxicity

Cited by 23 publications

References 54 publications

Gemcitabine-Vitamin E Prodrug-Loaded Micelles for Pancreatic Cancer Therapy

Gemcitabine-Vitamin E Prodrug-Loaded Micelles for Pancreatic Cancer Therapy

Magnetic nanosystem a tool for targeted delivery and diagnostic application: Current challenges and recent advancement

An approach for an enhanced anticancer activity of ferulic acid-loaded polymeric micelles via MicroRNA-221 mediated activation of TP53INP1 in caco-2 cell line

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