Chlorambucil Encapsulation into PLGA  Nanoparticles and Cytotoxic Effects in Breast Cancer Cell

Dias, Diego Juscelino Santos; Joanitti, Graziella Anselmo; Azevedo, Ricardo Bentes; Silva, Luciano; Lunardi, Claure N.; Gomes, Anderson J.

doi:10.4236/jbpc.2015.61001

Cited by 18 publications

(13 citation statements)

References 50 publications

(46 reference statements)

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“…L-Carnitine HCl started to melt around 220°C, and a sharp endothermic melting peak was detected at 250°C. Tg was observed at 50°C as mentioned in the literature (56,57). Thermograms of L-carnitine encapsulated and unloaded PLGA NPs revealed similar findings except that the endothermic melting peak of L-carnitine at 250°C became apparent in the case of encapsulated PLGA NPs.…”

Section: Thermal Behavior Of Nano-carnitine and Lipo-carnitine Structuressupporting

confidence: 81%

Polymeric Nanoparticle Versus Liposome Formulations: Comparative Physicochemical and Metabolomic Studies as l-Carnitine Delivery Systems

et al. 2020

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L-Carnitine has attracted much more attention especially in the treatment of crucial diseases such as diabetes, regional slimming, and obesity because of its metabolic activities. However, because of its short half-life, low bioavailability, and inability to be stored in the body, frequent dosing is required. In this study, L-carnitine-loaded liposome (lipocarnitine) and PLGA nanoparticle (nano-carnitine) formulations were prepared and characterized. For lipo-carnitine and nano-carnitine formulations, particle size values were 97.88 ± 2.96 nm and 250.90 ± 6.15 nm; polydispersity index values were 0.35 ± 0.01 and 0.22 ± 0.03; zeta potential values were 6.36 ± 0.54 mV and − 32.80 ± 2.26 mV; and encapsulation efficiency percentage values were 14.26 ± 3.52% and 21.93 ± 4.17%, respectively. Comparative in vitro release studies of novel formulations and solution of L-carnitine revealed that Lcarnitine released 90% of its content at the end of 1st hour. On the other hand, lipo-carnitine and nano-carnitine formulations maintained a controlled-release profile for 12 h. The in vitro efficacy of the formulations on cardiac fibroblasts (CFs) was evaluated by metabolomic studies and pathway analysis. Besides the prolonged release, lipo-carnitine/nano-carnitine formulations were also found to be effective on amino acid, carbohydrate, and lipid metabolisms. As a result, innovative nano-formulations were successfully developed as an alternative to conventional preparations which are available on the market.

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Section: Thermal Behavior Of Nano-carnitine and Lipo-carnitine Structuressupporting

confidence: 81%

Polymeric Nanoparticle Versus Liposome Formulations: Comparative Physicochemical and Metabolomic Studies as l-Carnitine Delivery Systems

et al. 2020

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“…e immediate fast release of berberine and C. citrinus extract could be attributed to rapid desorption and subsequent release from the outer boundary of PLGA nanoparticles as previously described during chlorambucil encapsulation [40]. All three treatments exhibited a similar pattern of release with encapsulated berberine being signi cantly higher than the other two treatments during the rst 7 days, while combination of berberine and C. citrinus release was signi cantly lower than the other two treatments during the remainder of the study period (Figure 4(a)).…”

Section: Percent Release Of Total Phenolics From Loadedmentioning

confidence: 53%

Poly(lactic-co-glycolic acid) Nanoparticles Loaded with Callistemon citrinus Phenolics Exhibited Anticancer Properties against Three Breast Cancer Cell Lines

Ahmed

Tariq

Ahmad

et al. 2019

Journal of Food Quality

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Fruit and vegetable diets rich in phenolic compounds reduce the risk of various cancers and offer multiple other health benefits due to their bioactivity and powerful antioxidant properties. However, the human health benefits of most phenolic compounds are restricted due to their limited aqueous solubility, low absorption, restricted passive cellular efflux, and poor gastrointestinal stability. Nanotechnology has been used to deliver various therapeutic drugs to specific targets overcoming many of the limitations of direct treatments. This study was designed to develop poly(lactic-co-glycolic acid) (PLGA) nanoencapsulated phenolic-rich extracts from Callistemon citrinus and berberine and to evaluate their effectiveness against extremely invasive MDA-MB 231, moderately invasive MCF-10A, and minimally invasive MCF-7 breast cancers. We have achieved about 80% encapsulation of phenolics from C. citrinus. Most encapsulated nanoparticles were polygonal with particles sizes of 200 to 250 nm. Release of phenolics from encapsulation during storage was biphasic during the first week and then levelled off thereafter. Nanoencapsulated phenolics from C. citrinus extract, berberine, and combination of both enhanced their bioactivity against the three breast cancer cell lines by nearly 2-fold. Growth inhibition of cells was a linear curve relative to phenolic concentration, with a maximum inhibition of nearly 100% at 0.1 mg/ml compared to control.

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“…Determination of the particle size of microspheres : Particle size of the prepared microspheres was measured using a dynamic light scattering particle size analyzer, model Zetasizer Nano-ZS, ZEN 3500, Malvern Instruments (Worcestershire, UK) at 25.0 ± 0.1°C[ 34 , 35 ]. Lyophilized microspheres (1 mg) were re-suspended in distilled water (100 mL) and the particle size was recorded in triplicate.…”

Section: Methodsmentioning

confidence: 99%

New hydrazonoindolin-2-ones: Synthesis, exploration of the possible anti-proliferative mechanism of action and encapsulation into PLGA microspheres

et al. 2017

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The synthesis and molecular characterization of new isatin-based hydrazonoindolin-2-ones 4a-o and 7a-e are reported. The in vitro anti-proliferative potential of the synthesized compounds 4a-o and 7a-e was examined against HT-29 (colon), ZR-75 (breast) and A549 (lung) human cancer cell lines. Compounds 7b, 7d and 7e were the most active congeners against the tested human cancer cell lines with average IC50 values of 4.77, 3.39 and 2.37 μM, respectively, as compared with the reference isatin-based drug, sunitinib, which exhibited an average IC50 value of 8.11 μM. Compound 7e was selected for further pharmacological evaluation in order to gain insight into its possible mechanism of action. It increased caspase 3/7 activity by 2.4- and 1.85-fold between 4 and 8 h of treatment, respectively, at 10 μM and it caused a decrease in the percentage of cells in the G1 phase of the cell cycle with a corresponding increase in the S-phase. In addition, compound 7e increased phosphorylated tyrosine (p-Tyr) levels nearly two-fold with an apparent IC50 value of 3.8 μM. The 7e-loaded PLGA microspheres were prepared using a modified emulsion-solvent diffusion method. The average encapsulation efficiency of the 7e-loaded PLGA microspheres was 85% ± 1.3. While, the in vitro release profile of the 7e-loaded microspheres was characterized by slow and continuous release of compound 7e during 21 days and the release curve was fitted to zero order kinetics. Incorporation of 7e into PLGA microspheres improved its in vitro anti-proliferative activity toward the human cancer cell line A549 after 120 h incubation period with an IC50 value less than 0.8 μM.

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Chlorambucil Encapsulation into PLGA Nanoparticles and Cytotoxic Effects in Breast Cancer Cell

Cited by 18 publications

References 50 publications

Polymeric Nanoparticle Versus Liposome Formulations: Comparative Physicochemical and Metabolomic Studies as l-Carnitine Delivery Systems

Polymeric Nanoparticle Versus Liposome Formulations: Comparative Physicochemical and Metabolomic Studies as l-Carnitine Delivery Systems

Poly(lactic-co-glycolic acid) Nanoparticles Loaded with Callistemon citrinus Phenolics Exhibited Anticancer Properties against Three Breast Cancer Cell Lines

New hydrazonoindolin-2-ones: Synthesis, exploration of the possible anti-proliferative mechanism of action and encapsulation into PLGA microspheres

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