Solid‐state Solubility Influences Encapsulation and Release of Hydrophobic Drugs from PLGA/PLA Nanoparticles

Panyam, Jayanth; Williams, D. S.; Dash, Alekha K.; Leslie‐Pelecky, Diandra L.; Labhasetwar, Vinod

doi:10.1002/jps.20094

Cited by 264 publications

(153 citation statements)

References 25 publications

Supporting

Mentioning

138

Contrasting

Unclassified

Order By: Relevance

“…This data is important because the presence of drug in molecular dispersion form helps in its sustained release. 36 This was further confirmed by the absence of a 5-FU peak in the X-ray diffractograms of the nanoparticle formulation (Figure 4). To analyze the dependence of PLGA combination on drug release, in vitro release studies were conducted.…”

mentioning

confidence: 57%

Biological evaluation of 5-fluorouracil nanoparticles for cancer chemotherapy and its dependence on the carrier, PLGA

K¹,

Jagadeeshan²,

Nair³

et al. 2011

IJN

View full text Add to dashboard Cite

Nanoscaled devices have great potential for drug delivery applications due to their small size. In the present study, we report for the first time the preparation and evaluation of antitumor efficacy of 5-fluorouracil (5-FU)-entrapped poly (D, L-lactic-co-glycolic acid) (PLGA) nanoparticles with dependence on the lactide/glycolide combination of PLGA. 5-FU-loaded PLGA nanoparticles with two different monomer combinations, 50-50 and 90-10 were synthesized using a modified double emulsion method, and their biological evaluation was done in glioma (U87MG) and breast adenocarcinoma (MCF7) cell lines. 5-FU-entrapped PLGA 50-50 nanoparticles showed smaller size with a high encapsulation efficiency of 66%, which was equivalent to that of PLGA 90-10 nanoparticles. Physicochemical characterization of nanoparticles using differential scanning calorimetry and X-ray diffraction suggested the presence of 5-FU in molecular dispersion form. In vitro release studies showed the prolonged and sustained release of 5-FU from nanoparticles with both the PLGA combinations, where PLGA 50-50 nanoparticles showed faster release. Nanoparticles with PLGA 50-50 combination exhibited better cytotoxicity than free drug in a dose- and time-dependent manner against both the tumor cell lines. The enhanced efficiency of PLGA 50-50 nanoparticles to induce apoptosis was indicated by acridine orange/ethidium bromide staining. Cell cycle perturbations studied using flow cytometer showed better S-phase arrest by nanoparticles in comparison with free 5-FU. All the results indicate that PLGA 50-50 nanoparticles possess better antitumor efficacy than PLGA 90-10 nanoparticles and free 5-FU. Since, studies have shown that long-term exposure of ailing tissues to moderate drug concentrations is more favorable than regular administration of higher concentration of the drug; our results clearly indicate the potential of 5-FU-loaded PLGA nanoparticles with dependence on carrier combination as controlled release formulation to multiplex the therapeutic effect of cancer chemotherapy.

show abstract

mentioning

confidence: 57%

Biological evaluation of 5-fluorouracil nanoparticles for cancer chemotherapy and its dependence on the carrier, PLGA

K¹,

Jagadeeshan²,

Nair³

et al. 2011

IJN

View full text Add to dashboard Cite

show abstract

“…Size exclusion chromatography [58][59][60] Surface chemistry analysis X-ray photoelectron spectroscopy 28,61,62 Fourier transform infrared spectroscopy 54,63,64 Nuclear magnetic resonance spectroscopy [64][65][66] Surface charge Zetasizer 56,67,68 Crystallinity X-ray diffraction 37,69,70 Differential scanning calorimetry [71][72][73] Hydrophobicity, hydrophilicity water contact angle measurements 65,74,75 Hydrophobic interaction chromatography [76][77][78] Drug entrapment efficiency, drug release studies…”

Section: Molecular Weightmentioning

confidence: 99%

Polylactide-co-glycolide nanoparticles for controlled delivery of anticancer agents

Dinarvand¹,

Sepehri²,

Manoochehri³

et al. 2011

IJN

396

265

View full text Add to dashboard Cite

The effectiveness of anticancer agents may be hindered by low solubility in water, poor permeability, and high efflux from cells. Nanomaterials have been used to enable drug delivery with lower toxicity to healthy cells and enhanced drug delivery to tumor cells. Different nanoparticles have been developed using different polymers with or without surface modification to target tumor cells both passively and/or actively. Polylactide-co-glycolide (PLGA), a biodegradable polyester approved for human use, has been used extensively. Here we report on recent developments concerning PLGA nanoparticles prepared for cancer treatment. We review the methods used for the preparation and characterization of PLGA nanoparticles and their applications in the delivery of a number of active agents. Increasing experience in the field of preparation, characterization, and in vivo application of PLGA nanoparticles has provided the necessary momentum for promising future use of these agents in cancer treatment, with higher efficacy and fewer side effects.

show abstract

“…Panyam et al 25 demonstrated that when hydrophobic drugs are used, NPs drug loading is closely matched with the respective solid-state drug-polymer solubility, that is, the ability of the polymeric matrix to entrap drug in the dispersed state. The solid-state solubility of the drug in the polymer increased with an increase in the lactide content in the polymer and with a decrease in the molecular weight.…”

Section: Drug Loadingmentioning

confidence: 99%

Cannabinoid derivate-loaded PLGA nanocarriers for oral administration: formulation, characterization, and cytotoxicity studies

Martín-Banderas¹,

Álvarez-Fuentes²,

Durán‐Lobato³

et al. 2012

IJN

View full text Add to dashboard Cite

CB13 (1-Naphthalenyl[4-(pentyloxy)-1-naphthalenyl]methanone)-loaded poly(lactic-co-glycolic acid) nanoparticles (NPs) were produced by nanoprecipitation and tested for their in vitro release behavior and in vitro cytotoxicity assays. The effects of several formulation parameters such as polymer type, surfactant concentration, and initial drug amount were studied. NPs had a particle size 90-300 nm in diameter. Results obtained show that the main influence on particle size was the type of polymer employed during the particle production: the greater the hydrophobicity, the smaller the particle size. In terms of encapsulation efficiency (%), high values were achieved (∼68%-90%) for all formulations prepared due to the poor solubility of CB13 in the external aqueous phase. Moreover, an inverse relationship between release rate and NP size was found. On the other hand, low molecular weight and low lactide content resulted in a less hydrophobic polymer with increased rates of water absorption, hydrolysis, and erosion. NPs showed no cytotoxicity and may be considered to be appropriate for drug-delivery purposes.

show abstract

Solid‐state Solubility Influences Encapsulation and Release of Hydrophobic Drugs from PLGA/PLA Nanoparticles

Cited by 264 publications

References 25 publications

Biological evaluation of 5-fluorouracil nanoparticles for cancer chemotherapy and its dependence on the carrier, PLGA

Biological evaluation of 5-fluorouracil nanoparticles for cancer chemotherapy and its dependence on the carrier, PLGA

Polylactide-co-glycolide nanoparticles for controlled delivery of anticancer agents

Cannabinoid derivate-loaded PLGA nanocarriers for oral administration: formulation, characterization, and cytotoxicity studies

Contact Info

Product

Resources

About