Strategies for encapsulation of small hydrophilic and amphiphilic drugs in PLGA microspheres: State-of-the-art and challenges

Ramazani, Farshad; Chen, Weiluan; Nostrum, Cornelus F. van; Storm, Gerrit; Kießling, Fabian; Lammers, Twan; Hennink, Wim E.; Kok, Robbert J.

doi:10.1016/j.ijpharm.2016.01.020

Cited by 232 publications

(157 citation statements)

References 80 publications

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“…They can maximize the embolic effect and angiogenesis inhibition, minimize the systemic toxicity of SOF, and monitor the lesion on follow-up CT imaging. PLGA has been widely used as a biocompatible and biodegradable polymer to prepare drug carriers 23, 24 . Considering its hydrophobic and degradable characteristics, it can be used for the fabrication of MSs and the sustained release of poorly water soluble drugs; as a result, biosafety can be accomplished 24 .…”

Section: Introductionmentioning

confidence: 99%

Sorafenib and 2,3,5-triiodobenzoic acid-loaded imageable microspheres for transarterial embolization of a liver tumor

Choi

Park

Cho

et al. 2017

Sci Rep

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Sorafenib (SOF; an angiogenesis inhibitor) and 2,3,5-triiodobenzoic acid (TIBA; a contrast agent for computed tomography imaging)-loaded poly(lactic-co-glycolic acid) (PLGA) microspheres (MSs) were fabricated. Embolization, drug delivery, and tracing the distribution of MSs for liver cancer therapy were accomplished with the developed MSs after their intra-arterial (IA) administration. SOF/TIBA/PLGA MSs with 24.8–28.5 µm mean diameters were prepared, and the sustained release of SOF from MSs was observed. Lower systemic exposure (represented as the area under the curve [AUC]) and maximum drug concentration in plasma (Cmax) values of the SOF/TIBA/PLGA MSs group (IA administration, 1 mg/kg) in the results of the pharmacokinetic study imply alleviated unwanted systemic effects (e.g., hand and foot syndrome), compared to the SOF solution group (oral administration, 10 mg/kg). In a rat hepatoma model, the increase of microvessel density (MVD) following arterial embolization (i.e., reactive angiogenesis) was partially limited by SOF/TIBA/PLGA MSs. This resulted in the SOF/TIBA/PLGA MSs group (IA administration, single dosing, 1 mg/kg) showing a smaller tumor size increase and viable tumor portion compared to the TIBA/PLGA MSs group. These findings suggest that a developed SOF/TIBA/PLGA MS can be a promising therapeutic system for liver cancer using a transarterial embolization strategy.

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Section: Introductionmentioning

confidence: 99%

Sorafenib and 2,3,5-triiodobenzoic acid-loaded imageable microspheres for transarterial embolization of a liver tumor

Choi

Park

Cho

et al. 2017

Sci Rep

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“…It would be premature to conclude that no beneficial effects will be seen if the treatment were given for less than three months or if another administration route were used. There are subcutaneously injected sustained slow-release formulations used clinically, including polymeric slow release microspheres, which might be explored for further development of EUK-207 [52]. If long time periods are needed to mitigate CNS radiation-induced cognitive injury, such formulations might be most convenient for treating larger exposed populations after a radiological accident or terrorism event because a single subcutaneous injection would enable drug release for a prolonged period.…”

Section: Discussionmentioning

confidence: 99%

Mitigating effect of EUK-207 on radiation-induced cognitive impairments

Raber

Davis

Pfankuch

et al. 2017

Behavioural Brain Research

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The brain could be exposed to irradiation as part of a nuclear accident, radiological terrorism (dirty bomb scenario) or a medical radiological procedure. In the context of accidents or terrorism, there is considerable interest in compounds that can mitigate radiation-induced injury when treatment is initiated a day or more after the radiation exposure. As it will be challenging to determine the radiation exposure an individual has received within a relatively short time frame, it is also critical that the mitigating agent does not negatively affect individuals, including emergency workers, who might be treated, but who were not exposed. Alterations in hippocampus-dependent cognition often characterize radiation-induced cognitive injury. The catalytic ROS scavenger EUK-207 is a member of the class of metal-containing salen manganese (Mn) complexes that suppress oxidative stress, including in the mitochondria, and have been shown to mitigate radiation dermatitis, promote wound healing in irradiated skin, and mitigate vascular injuries in irradiated lungs. As the effects of EUK-207 against radiation injury in the brain are not known, we assessed the effects of EUK-207 on sham-irradiated animals and the ability of EUK-207 to mitigate radiation-induced cognitive injury. The day following irradiation or sham-irradiation, the mice started to receive EUK-207 and were cognitively tested 3 months following exposure. Mice irradiated at a dose of 15 Gy showed cognitive impairments in the water maze probe trial. EUK-207 mitigated these impairments while not affecting cognitive performance of sham-irradiated mice in the water maze probe trial. Thus, EUK-207 has attractive properties and should be considered an ideal candidate to mitigate radiation-induced cognitive injury.

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“…us, the development of carriers to transport and stabilize NAC inside the body is a major concern when researching for new ways to increase its bioavailability. In this scenario, nanoparticles manufactured in materials such as PLGA, a biodegradable copolymer, are being developed [7][8][9].…”

Section: Introductionmentioning

confidence: 99%

“…Entrapping low molecular weight hydrophilic compounds, like NAC in PLGA nanoparticles, represents a challenge as the small size of the substance facilitates its migration and rapid release [7,10].…”

Section: Introductionmentioning

confidence: 99%

Improvement of N-Acetylcysteine Loaded in PLGA Nanoparticles by Nanoprecipitation Method

Lancheros

Guerrero

Godoy-Silva

2018

Journal of Nanotechnology

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N-Acetylcysteine (NAC) is a hydrophilic compound with a low bioavailability. It has been used as an effective antioxidant agent.is research seeks to enhance the entrapment of NAC in PLGA nanoparticles for drug delivery systems. e nanoparticles were made using the nanoprecipitation method and changing the following parameters: the solvent/nonsolvent nature, its viscosity, pH, NAC addition to the nonsolvent, the polymer concentration and molecular weight, and NAC concentration in the solvent.e results showed that an increase in the nonsolvent viscosity produces NAC concentration in the solvent, and the nonsolvent rises its entrapment in the nanoparticles. Nanoparticles with 235.5 ± 11.4 nm size with an entrapment efficiency of 0.4 ± 0.04% and a specific load of 3.14 ± 0.33% were obtained. e results suggest that besides efficiently entrapping hydrophobic compounds, the nanoprecipitation method also has a high potential as an alternative entrapment method for hydrophilic compounds as well. However, its use in the pharmaceutical industry, as a proper specific load vehicle, still depends on the improvement of the load capacity.

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Strategies for encapsulation of small hydrophilic and amphiphilic drugs in PLGA microspheres: State-of-the-art and challenges

Cited by 232 publications

References 80 publications

Sorafenib and 2,3,5-triiodobenzoic acid-loaded imageable microspheres for transarterial embolization of a liver tumor

Sorafenib and 2,3,5-triiodobenzoic acid-loaded imageable microspheres for transarterial embolization of a liver tumor

Mitigating effect of EUK-207 on radiation-induced cognitive impairments

Improvement of N-Acetylcysteine Loaded in PLGA Nanoparticles by Nanoprecipitation Method

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