-
[show abstract]
[hide abstract]
ABSTRACT: In this paper, novel cyclosporine A (CsA)-loaded amphiphilic poly(L-aspartic acid-co-L-lactic acid) (PAL)-1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine (DPPE) copolymer nanoparticles (NPs) were successfully fabricated using an emulsion/solvent evaporation technique. The CsA-loaded NPs were characterized by dynamic light scattering (DLS) and transmission electron microscopy (TEM). The CsA-loaded NPs size, size distribution, encapsulation efficiency (EE) and drug-loading content (LC) were influenced by polyvinyl alcohol (PVA) concentration and the weight ratio of the copolymer to CsA. In vitro release behavior of CsA-loaded NPs showed a sustained release. With the increasing of copolymer/CsA weight ratio, the release of CsA from NPs is rapid. The poly(L-aspartic acid) derivatives NPs have a promising potential in hydrophobic drug delivery system.
Journal of Nanoscience and Nanotechnology 02/2013; 13(2):1444-7. · 1.56 Impact Factor
-
[show abstract]
[hide abstract]
ABSTRACT: Novel biodegradable amphiphilic copolymer nanoparticles based on gelatin, poly(lactide) and 1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine (DPPE) (gelatin-co-PLA-DPPE) have been successfully fabricated. In order to estimate the feasibility as drug carriers, an anti-tumor model drug doxorubicin hydrochloride salt (DOX) was incorporated into polymeric nanoparticles by double emulsion or nanoprecipitation method. The nanoparticle size, size distribution and encapsulation efficiency (EE) were influenced by the feed weight ratio of the copolymer to DOX and different fabrication methods of nanoparticles. In addition, in vitro release experiments exhibited the release behavior was affected by pH of release media. The DOX-loaded nanoparticles showed that faster release at pH 5.0 than their release at pH 7.4 buffer. The DOX-loaded copolymer nanoparticles showed comparable anticancer efficacy with the free drug in vitro and in vivo. These results demonstrate a feasible application of the gelatin derivative as a promising nanocarrier for delivery of anti-tumor drugs.
Colloids and surfaces. B, Biointerfaces 09/2012; 102C:833-841. · 2.60 Impact Factor
-
[show abstract]
[hide abstract]
ABSTRACT: A novel poly(l-aspartic) derivative (PAL-DPPE) containing polylactide and 1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine (DPPE) segments
has been successfully synthesized. The chemical structures of the copolymers were confirmed by Fourier-transform infrared
spectroscopy (FTIR), NMR (1H NMR, 13C NMR, 31P NMR), and thermogravimetric analysis (TGA). Fluorescence spectroscopy, dynamic light scattering (DLS), and transmission
electron microscopy (TEM) confirmed the formation of micelles of the PAL-DPPE copolymers. In order to estimate the feasibility
as novel drug carriers, an anti-tumor model drug doxorubicin (DOX) was incorporated into polymeric micelles by double emulsion
and nanoprecipitation method. The DOX-loaded micelle size, size distribution, and encapsulation efficiency (EE) were influenced
by the feed weight ratio of the copolymer to DOX. In addition, in vitro release experiments of the DOX-loaded PAL-DPPE micelles
exhibited that faster release in pH 5.0 than their release in pH 7.4 buffer. The poly(l-aspartic) derivative copolymer was proved to be an available carrier for the preparation of micelles for anti-tumor drug
delivery.
Keywords
l-Aspartic acid–Polylactide–1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine–Nanoparticles–Doxorubicin delivery system–Nanomedicine
Journal of Nanoparticle Research 05/2012; 13(9):4371-4385. · 3.29 Impact Factor
-
[show abstract]
[hide abstract]
ABSTRACT: The use of biodegradable polymeric nanoparticles (NPs) for controlled drug delivery has shown significant therapeutic potential. Polyaspartic acid and polylactic acid are the most intensively studied biodegradable polymers. In the present study, novel amphiphilic biodegradable co-polymer NPs, poly(L-aspartic acid-co-lactic acid) with 1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine (DPPE) (poly(AA-co-LA)/DPPE) is synthesized and subsequently used to encapsulate an antitumor drug doxorubicin (DOX). The formulation parameters of the NPs are optimized to improve encapsulation efficiency. The resulting drug-loaded NPs possess better size homogeneity (polydispersity) and exhibit pH-responsive drug release profiles. Cellular viability assays indicate that the poly(AA-co-LA)/DPPE NPs did not induce cell death, whereas doxorubicin encapsulated NPs were cytotoxic to various types of tumor cells. In addition, the free NPs could not enter the cell nuclei after internalized in tumor cells. The DOX-loaded NPs exhibit efficient intracellular delivery in tumor cells with co-localization in lysosome and delay entering into the nucleus, which suggests a time- and pH-dependent drug release profile within cells. When applied to deliver chemotherapeutics to a mouse xenograft model of human lung adenocarcinoma, DOX-loaded NPs have a comparable antitumor activity with free DOX, and greatly reduce systemic toxicity and mortality. The delivery of cytotoxic drugs directly to the nucleus specifically within tumor cells is of great interest. These results demonstrate the feasibility of the application of the amphiphilic polyaspartic acid derivative, poly(AA-co-LA)/DPPE, as a nanocarrier for cell nuclear delivery of potent antitumor drugs.
Small 03/2012; 8(10):1596-606. · 8.35 Impact Factor
-
[show abstract]
[hide abstract]
ABSTRACT: Novel amphiphilic copolymer nanoparticles (HPAE-co-PLA-DPPE) composed of hyperbranched poly (amine-ester), polylactide and 1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine (DPPE) segments were designed and synthesized that provided high encapsulation efficiency. These nanoparticles (NPs) were used to encapsulate an antitumor model drug, doxorubicin (DOX). The resulting NPs exhibited high encapsulation efficiency to DOX under an appropriate condition. In vitro release experiments revealed that the release of DOX from NPs was faster at pH 4.5 than that at pH 7.4 or pH 6.0. Confocal microscopy observation indicated that the DOX-loaded NPs can enter cells and localize in lysosomes that can be released quickly into the cytoplasm. The DOX-loaded NPs showed comparable anticancer efficacy with the free drug both in vivo and in vitro. These results demonstrate a feasible application of the hyperbranched copolymer, HPAE-co-PLA-DPPE, as a promising nanocarrier for intracellular delivery of antitumor drugs. FROM THE CLINICAL EDITOR: In this paper, the development of novel amphiphilic copolymer nanoparticles is discussed with the goal of establishing high encapsulation efficiency for chemotherapy drugs.
Nanomedicine: nanotechnology, biology, and medicine 05/2011; 7(6):945-54. · 5.44 Impact Factor
-
[show abstract]
[hide abstract]
ABSTRACT: A novel amphiphilic copolymer based on dextran, poly(lactide) (PLA) and 1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine (DPPE) was synthesized and characterized by FT-IR, 1H NMR, 13C NMR and 31P NMR spectra. Their molecular weights were determined by gel permeation chromatography (GPC). The molecular weights range from 30 000 g mol−1 to 37 000 g mol−1 with a feed weight ratio of 20:1–50:1 (DPPE/activated dextran–PLA). Its micellar characteristics were investigated using fluorescence technique, transmission electron microscopy (TEM) and dynamic light scattering (DLS). It was found that dextran–PLA–DPPE copolymer could form spherical micelles. The micelle diameters ranged from 85 to 120 nm with a feed weight ratio of 20:1–50:1 (DPPE/activated dextran–PLA) in the absence of surfactant.
Carbohydrate Polymers 83(3):1408-1413. · 3.63 Impact Factor
