In past two decades poly lactic-co-glycolic acid (PLGA) has been among the most attractive polymeric candidates used to fabricate devices for drug delivery and tissue engineering applications. PLGA is biocompatible and biodegradable, exhibits a wide range of erosion times, has tunable mechanical properties and most importantly, is a FDA approved polymer. In particular, PLGA has been extensively studied for the development of devices for controlled delivery of small molecule drugs, proteins and other macromolecules in commercial use and in research. This manuscript describes the various fabrication techniques for these devices and the factors affecting their degradation and drug release.

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Poly Lactic-co-Glycolic Acid (PLGA) as Biodegradable Controlled Drug Delivery Carrier

Nanoparticles in cancer therapy and diagnosis

Nanoparticle (NP) drug delivery systems (5−250 nm) have the potential to improve current disease therapies because of their ability to overcome multiple biological barriers and releasing a therapeutic load in the optimal dosage range. Rapid clearance of circulating nanoparticles during systemic delivery is a critical issue for these systems and has made it necessary to understand the factors affecting particle biodistribution and blood circulation half-life. In this review, we discuss the factors which can influence nanoparticle blood residence time and organ specific accumulation. These factors include interactions with biological barriers and tunable nanoparticle parameters, such as composition, size, core properties, surface modifications (pegylation and surface charge), and finally, targeting ligand functionalization. All these factors have been shown to substantially affect the biodistribution and blood circulation half-life of circulating nanoparticles by reducing the level of nonspecific uptake, de...

http://pubs.acs.org/doi/pdf/10.1021/mp800051m

Factors Affecting the Clearance and Biodistribution of Polymeric Nanoparticles

PEGylation as a strategy for improving nanoparticle-based drug and gene delivery

PEGylated PLGA nanoparticles as protein carriers: synthesis, preparation and biodistribution in rats

PEGylated polycyanoacrylate nanoparticles as tumor necrosis factor-α carriers

The objective of this study was to investigate the pharmacokinetics and in vivo anti-tumor effect of recombinant human tumor necrosis factor-α (rHuTNF-α) encapsulated in poly(methoxypolyethyleneglycol cyanoacrylate-co-n-hexadecyl cyanoacrylate) (PEG-PHDCA) nanoparticles. Our experimental results showed that PEG-PHDCA nanoparticles could extend the half-life of rHuTNF-α to 7.42 h and obviously change the protein biodistribution in tissues, and in particular, increase accumulation of rHuTNF-α in tumor. Compared with PHDCA nanoparticles and free rHuTNF-α, PEG-PHDCA nanoparticles loaded with rHuTNF-α showed higher anti-tumor potency at the same dose, which might be related to its higher accumulation in tumor tissues and longer plasma circulation time. Therefore, PEG-PHDCA nanoparticles could be an effective carrier for rHuTNF-α.

https://www.jstage.jst.go.jp/article/bpb/24/6/24_6_662/_pdf

Stealth Polycyanoacrylate Nanoparticles as Tumor Necrosis Factor-α Carriers: Pharmacokinetics and Anti-tumor Effects

Aim: To assess the merits of polyethylene glycol-modified recombinant human tumor necrosis factor alpha (PEG-rHuTNF-alpha).
 Methods: The rHuTNF-alpha was modified with N-succinimidyl succinate monomethoxy polyethylene glycol (SS-PEG) of three different molecular weights. The PEG-rHuTNF-alpha was separated into fractions of various molecular weights by gel filtration chromatography. In vitro activities of various fractions were determined with L929 cell assay and in vivo anti-tumor potencies of main fractions were studied with respect to necrosis of S-180 solid tumor.
 Results: The rHuTNF-alpha could be modified using SS-PEG under mild conditions. The main fraction of PEG5000-rHuTNF-alpha contained four PEG molecules, and PEG12000-rHuTNF-alpha and PEG20000-rHuTNF-alpha contained two PEG molecules, respectively. There was a higher activity when rHuTNF-alpha was coupled to less numbers of the same molecular weight PEG molecules. When PEG-rHuTNF-alpha was of the same molecular weight, rHuTNF-alpha modified with bigger molecular weight PEG molecules had a higher activity. PEG-rHuTNF-alpha was resistant to proteolysis, and over 70 % activity remained after 8 h, but the activity of rHuTNF-alpha was time-dependently diminished by incubation with bovine trypsin. PEG5000-rHuTNF-alpha (1500 IU per mouse) had a similar anti-tumor potency compared with rHuTNF-alpha (3000 IU per mouse). PEG12000-rHuT NF-alpha (1500 IU per mouse) had an increased anti-tumor potency compared with rHuTNF-alpha (3000 IU per mouse). In particular, PEG20000-rHuTNF-alpha at a dose of 1500 IU per mouse had a higher anti-tumor potency than rHuTNF-alpha at a dose of 6000 IU per mouse.
 Conclusion: PEG-modified rHuTNF-alpha could be more suitable for therapeutic use

PEGylated recombinant human tumor necrosis factor alpha: preparation and anti-tumor potency.

AIM:
To prepare and identify ipriflavone (IP) solid dispersion, and determine its dissolution property.
METHODS:
The solvent method was used for preparation and differential scanning calorimetry (DSC), X-ray diffraction and infrared spectrophotometry for identification of IP solid dispersion. The dissolution of the dispersion was determined with paddle method.
RESULTS:
The dissolution of IP solid dispersion consisting of IP and povidone-k30 (PVP) (1:8) in artificial gastric juice is 6.15 times as high as that of IP alone. The DSC curves, X-ray diffraction patterns and infrared spectrophotometries of IP have been changed obviously by the dispersion.
CONCLUSION:
The dissolution of IP is increased by solid dispersion method.

Jian-Jun Zhou

Papers

PEGylated PLGA nanoparticles as protein carriers: synthesis, preparation and biodistribution in rats

PEGylated polycyanoacrylate nanoparticles as tumor necrosis factor-α carriers

Stealth Polycyanoacrylate Nanoparticles as Tumor Necrosis Factor-α Carriers: Pharmacokinetics and Anti-tumor Effects

PEGylated recombinant human tumor necrosis factor alpha: preparation and anti-tumor potency.

Preparation and dissolution property of ipriflavone solid dispersion.