An ion pairing approach to increase the loading of hydrophilic and lipophilic drugs into PEGylated PLGA nanoparticles

Dalwadi, Gautam; Sunderland, Bruce

doi:10.1016/j.ejpb.2008.08.004

Cited by 27 publications

(29 citation statements)

References 36 publications

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“…Despite the presence of DS in the SLN formulation, the average particle size monotonically decreased. This was as a result of higher amphiphilic properties and reduced interfacial tension between interfaces [47].…”

Section: Page 14 Of 42mentioning

confidence: 99%

Galactose engineered solid lipid nanoparticles for targeted delivery of doxorubicin

Jain

Kesharwani

Garg

et al. 2015

Colloids and Surfaces B: Biointerfaces

141

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Section: Page 14 Of 42mentioning

confidence: 99%

Galactose engineered solid lipid nanoparticles for targeted delivery of doxorubicin

Jain

Kesharwani

Garg

et al. 2015

Colloids and Surfaces B: Biointerfaces

141

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“…Thus, the combined effect of MW and amphiphilicity largely contributed to the reduction in particle size. 33 The high entrapment efficiency obtained (75%-90%) for both PLGA and PLGA-PEG NSs could be explained by the hydrophobic nature of FB. The presence of hydrophilic PEG segments resulted in lower entrapment efficiency values in comparison with PLGA NSs.…”

Section: Nss Characterizationmentioning

confidence: 99%

Role of hydroxypropyl-β-cyclodextrin on freeze-dried and gamma-irradiated PLGA and PLGA–PEG diblock copolymer nanospheres for ophthalmic flurbiprofen delivery

Vega¹,

Egea²,

Calpena³

et al. 2012

IJN

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Poly(D,L-lactide-co-glycolide) and poly(D,L-lactide-co-glycolide) with poly(ethylene glycol) nanospheres (NSs) incorporating flurbiprofen (FB) were freeze-dried with several cryoprotective agents and sterilized by γ-irradiation. Only when 5.0% (w/v) hydroxypropyl-β-cyclodextrin (HPβCD) was used, a complete resuspension by manual shaking and almost identical particle size of the NSs was obtained after freeze-drying. In vitro drug release and ex vivo corneal permeation of NSs with and without HPβCD were evaluated. The presence of HPβCD resulted in a reduction of burst effect, providing a more sustained release of the drug. A significant decrease in the FB transcorneal permeation of NSs containing HPβCD was obtained, related to the slower diffusion of FB observed in the in vitro results. The uptake mechanism of the NSs was examined by confocal microscopy, suggesting that NSs penetrate corneal epithelium through a transcellular pathway. Ocular tolerance was assessed in vitro and in vivo by the Eytex™ and Draize test, respectively. Long-term stability studies revealed that γ-irradiated NSs stored as freeze-dried powders maintained their initial characteristics. Stability studies of the resuspended NSs after 3 months of storage in the aqueous form showed that NSs were stable at 4°C, while formulations stored at 25°C and 40°C increased their initial particle size.

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“…Dextran sulfate is a polyanionic derivative of dextran (a polymer of anhydroglucose) and has been utilized in various pharmaceutical formulations. 38,39 Finally, nanoparticles were characterized and compared for their size, morphology, and especially drug loading, drug entrapment efficiency, and in vitro drug release profile. In addition, the antibacterial effect of nanoparticles against standard Aggregatibacter actinomycetemcomitans, the most important pathogen in periodontal infections, was investigated in vitro.…”

Section: Introductionmentioning

confidence: 99%

Improved drug loading and antibacterial activity of minocycline-loaded PLGA nanoparticles prepared by solid/oil/water ion pairing method

Dinarvand¹,

Kashi²,

Eskandarion³

et al. 2012

IJN

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Background: Low drug entrapment efficiency of hydrophilic drugs into poly(lactic-co-glycolic acid) (PLGA) nanoparticles is a major drawback. The objective of this work was to investigate different methods of producing PLGA nanoparticles containing minocycline, a drug suitable for periodontal infections. Methods: Different methods, such as single and double solvent evaporation emulsion, ion pairing, and nanoprecipitation were used to prepare both PLGA and PEGylated PLGA nanoparticles. The resulting nanoparticles were analyzed for their morphology, particle size and size distribution, drug loading and entrapment efficiency, thermal properties, and antibacterial activity. Results: The nanoparticles prepared in this study were spherical, with an average particle size of 85-424 nm. The entrapment efficiency of the nanoparticles prepared using different methods was as follows: solid/oil/water ion pairing (29.9%) . oil/oil (5.5%) . water/oil/water (4.7%) . modified oil/water (4.1%) . nano precipitation (0.8%). Addition of dextran sulfate as an ion pairing agent, acting as an ionic spacer between PEGylated PLGA and minocycline, decreased the water solubility of minocycline, hence increasing the drug entrapment efficiency. Entrapment efficiency was also increased when low molecular weight PLGA and high molecular weight dextran sulfate was used. Drug release studies performed in phosphate buffer at pH 7.4 indicated slow release of minocycline from 3 days to several weeks. On antibacterial analysis, the minimum inhibitory concentration and minimum bactericidal concentration of nanoparticles was at least two times lower than that of the free drug. Conclusion: Novel minocycline-PEGylated PLGA nanoparticles prepared by the ion pairing method had the best drug loading and entrapment efficiency compared with other prepared nanoparticles. They also showed higher in vitro antibacterial activity than the free drug.

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An ion pairing approach to increase the loading of hydrophilic and lipophilic drugs into PEGylated PLGA nanoparticles

Cited by 27 publications

References 36 publications

Galactose engineered solid lipid nanoparticles for targeted delivery of doxorubicin

Galactose engineered solid lipid nanoparticles for targeted delivery of doxorubicin

Role of hydroxypropyl-β-cyclodextrin on freeze-dried and gamma-irradiated PLGA and PLGA–PEG diblock copolymer nanospheres for ophthalmic flurbiprofen delivery

Improved drug loading and antibacterial activity of minocycline-loaded PLGA nanoparticles prepared by solid/oil/water ion pairing method

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An ion pairing approach to increase the loading of hydrophilic and lipophilic drugs into PEGylated PLGA nanoparticles

Cited by 27 publications

References 36 publications

Galactose engineered solid lipid nanoparticles for targeted delivery of doxorubicin

Galactose engineered solid lipid nanoparticles for targeted delivery of doxorubicin

Role of hydroxypropyl-&beta;-cyclodextrin on freeze-dried and gamma-irradiated PLGA and PLGA&ndash;PEG diblock copolymer nanospheres for ophthalmic flurbiprofen delivery

Improved drug loading and antibacterial activity of minocycline-loaded PLGA nanoparticles prepared by solid/oil/water ion pairing method

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Role of hydroxypropyl-β-cyclodextrin on freeze-dried and gamma-irradiated PLGA and PLGA–PEG diblock copolymer nanospheres for ophthalmic flurbiprofen delivery