Multidrug Resistance for Cancer Treatment: Delivery of Ursolic Acid and Caffeine by Poly (Lactic-Co-Glycolic Acid) Nanoparticles

Merlin, J. P. Jose; Venkadesh, B.; Rajan, Sheeja S; Subramanian, Perumal

doi:10.4172/2572-4126.1000113

Cited by 3 publications

(4 citation statements)

References 30 publications

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“…By analyzing the data, we confirmed the anticancer potentials of Cf in safe doses (due to the polyphenolic acids, phenolic compounds and alkaloids) [ 41 , 56 ]. The increase in the cytotoxicity of Cf by nano-encapsulation within PLGA matrix provided three additional mechanisms over the non-encapsulated form, i.e., the selective cellular uptake (endocyto-sis) of the PLGA NPs into the cancerous cell lines (reported previously with different types of cancer cell lines such as breast (MCF-7) [ 42 ] and lung cancers (A-549) [ 57 ]), the im-proved release of the extract from the NPs (since MTT assay was performed on pure Cf and PLGA-Cf suspended in water), and finally, the inhibition of efflux transport ( p -glycoprotein) by PLGA, allowing more extract to be safely internalized and indwelled [ 57 ].…”

Section: Discussionmentioning

confidence: 62%

“…A further band found at 1600.92 cm −1 confirmed the conjugation since it referred to the presence of an aromatic alkene (–C=C–). Below 1600.00 m −1 , there was a band at 1238.30 cm −1 which might indicate the C–O stretch while the band at 1080.14 cm −1 might refer to C–N stretching [ 41 , 45 ]. On the contrary, the FT-IR spectra of both the unloaded and loaded PLGA NPs ( Figure 4 , PLGA NPs and PLGA-Cf-F 2 , respectively) showed the typical bands of PLGA [ 46 ] entailing the successful and complete inclusion of Cf extract within the PLGA matrix [ 19 , 47 ].…”

Section: Resultsmentioning

confidence: 99%

“…Finally, the LC% was determined from Equation (3). This method was performed according to previously applied protocols [ 18 , 19 , 38 , 39 , 40 , 41 , 42 ].

…”

Section: Methodsmentioning

confidence: 99%

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Applying Box–Behnken Design for Formulation and Optimization of PLGA-Coffee Nanoparticles and Detecting Enhanced Antioxidant and Anticancer Activities

et al. 2021

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In an attempt to prove biological activity enhancement upon particle size reduction to the nanoscale, coffee (Cf) was chosen to be formulated into poly(lactic-co-glycolic) acid (PLGA) nanoparticles (NPs) using the single emulsion-solvent evaporation (SE-SE) method via Box–Behnken Design (BBD) to study the impact of certain process and formulation parameters on the particle size and size homogeneity, surface stability and encapsulation efficiency (EE%). The coffee-loaded PLGA (PLGA-Cf) NPs were characterized by different methods to aid in selecting the optimum formulation conditions. The desirable physicochemical characteristics involved small particle sizes with an average of 318.60 ± 5.65 nm, uniformly distributed within a narrow range (PDI of 0.074 ± 0.015), with considerable stability (Zeta Potential of −20.50 ± 0.52 mV) and the highest EE% (85.92 ± 4.01%). The antioxidant and anticancer activities of plain PLGA NPs, pure Cf and the optimum PLGA-Cf NPs, were evaluated using 2,2-Diphenyl-1-picryl-hydrazyl (DPPH) and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assays, respectively. As a result of nano-encapsulation, antioxidant activity was enhanced by 26.5%. Encapsulated Cf showed higher anticancer potency than pure Cf against different cancerous cell lines with an increase of 86.78%, 78.17%, 85.84% and 84.84% against MCF-7, A-549, HeLa and HepG-2, respectively. The in vitro release followed the Weibull release model with slow and biphasic release profile in both tested pH media, 7.4 and 5.5.

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Section: Discussionmentioning

confidence: 62%

Section: Resultsmentioning

confidence: 99%

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Applying Box–Behnken Design for Formulation and Optimization of PLGA-Coffee Nanoparticles and Detecting Enhanced Antioxidant and Anticancer Activities

et al. 2021

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“…An encapsulation efficiency between 43.1% to 47.5% was achieved for ursolic acid with the reported preparation method. According to the literature, a very similar UA nanoparticle preparation procedure was presented by Merlin et al, where the researchers obtained nanoparticles with similar size and PDI values, but higher encapsulation efficiency, probably due to the use of a different method of determining UA concentration, with HPLC being recognized as a more accurate method for measuring non-chromophore rich compounds [ 59 ]. According to the literature, PLGA based nanoparticles are characterized by negative values of zeta potential, which are considered suitable for intravenous dosage.…”

Section: Discussionmentioning

confidence: 99%

Evaluation of the In Vitro Cytotoxic Activity of Ursolic Acid PLGA Nanoparticles against Pancreatic Ductal Adenocarcinoma Cell Lines

et al. 2021

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Among all the types of cancer, Pancreatic Ductal Adenocarcinoma remains one of the deadliest and hardest to fight and there is a critical unmet need for new drugs and therapies for its treatment. Naturally derived compounds, such as pentacyclic triterpenoids, have gathered attention because of their high cytotoxic potential towards pancreatic cancer cells, with a wide biological activity spectrum, with ursolic acid (UA) being one of the most interesting. However, due to its minimal water solubility, it is necessary to prepare a nanocarrier vehicle to aid in the delivery of this compound. Poly(lactic-co-glycolic acid) or PLGA polymeric nanocarriers are an essential tool for ursolic acid delivery and can overcome the lack in its biological activity observed after incorporating within liposomes. We prepared UA-PLGA nanoparticles with a PEG modification, to achieve a long circulation time, by using a nanoprecipitation method and subsequently performed an MTT cytotoxicity assay towards AsPC-1 and BxPC-3 cells, with TEM visualization of the nanoparticles and their cellular uptake. We established repeatable preparation procedures of the nanoparticles and achieved biologically active nanocarriers with an IC50 below 30 µM, with an appropriate size for intravenous dosage (around 140 nm), high sample homogeneity (below 0.2) and reasonable encapsulation efficiency (up to 50%). These results represent the first steps in the development of potentially effective PDAC therapies based on novel biologically active and promising triterpenoids.

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Hyperthermic Agent Prepared by One-Pot Modification of Maghemite Using an Aliphatic Polyester Model

et al. 2018

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Multidrug Resistance for Cancer Treatment: Delivery of Ursolic Acid and Caffeine by Poly (Lactic-Co-Glycolic Acid) Nanoparticles

Cited by 3 publications

References 30 publications

Applying Box–Behnken Design for Formulation and Optimization of PLGA-Coffee Nanoparticles and Detecting Enhanced Antioxidant and Anticancer Activities

Applying Box–Behnken Design for Formulation and Optimization of PLGA-Coffee Nanoparticles and Detecting Enhanced Antioxidant and Anticancer Activities

Evaluation of the In Vitro Cytotoxic Activity of Ursolic Acid PLGA Nanoparticles against Pancreatic Ductal Adenocarcinoma Cell Lines

Hyperthermic Agent Prepared by One-Pot Modification of Maghemite Using an Aliphatic Polyester Model

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