Nanocarriers for intravenous injection—The long hard road to the market

Wacker, Matthias G.

doi:10.1016/j.ijpharm.2013.08.079

Cited by 147 publications

(92 citation statements)

References 126 publications

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“…Subsequently, the entrapped ATM released from the core of the nanoparticles in a sustained manner due to the diffusion of drug across the albumin matrix, would provide the possibility of continual drug effect. A similar phenomenon was observed previously in albumin nanoparticles [69][70][71]. However the association of the drug with the carrier material in competition with other carriers such as plasma proteins, lipids, and cell membranes plays an important role for the performance in vivo [72].…”

Section: Discussionsupporting

confidence: 79%

Bio-inspired artemether-loaded human serum albumin nanoparticles for effective control of malaria-infected erythrocytes

Sidhaye¹,

Bhuran²,

Zambare³

et al. 2016

Nanomedicine

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Aim: The intra-erythrocytic development of the malarial parasite is dependent on active uptake of nutrients, including human serum albumin (HSA), into parasitized red blood cells (pRBCs). We have designed HSA-based nanoparticles as a potential drug-delivery option for antimalarials. Methods: Artemether-loaded nanoparticles (AAN) were designed and antimalarial activity evaluated in-vitro/in-vivo using Plasmodium falciparum/Plasmodium berghei species, respectively. Results: Selective internalisation of AAN into Plasmodiuminfected RBCs in preference to healthy erythrocytes was observed using confocal-imaging.In-vitro studies showed 50% dose reduction for AAN as compared to drug-only controls to achieve IC50 levels of inhibition. The nanoparticles exhibited 2-fold higher peak drug concentrations in RBCs with antimalarial activity at 50% of therapeutic doses in P.bergeiinfected mice. Conclusion: HSA-based nanoparticles offer safe and effective approach for selective targeting of antimalarial drugs.

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Section: Discussionsupporting

confidence: 79%

Bio-inspired artemether-loaded human serum albumin nanoparticles for effective control of malaria-infected erythrocytes

Sidhaye¹,

Bhuran²,

Zambare³

et al. 2016

Nanomedicine

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“…These findings stem from the fact that larger cubosomes would increase the drug diffusional distance and consequently slow down the drug dissolution rates (Wacker, 2013). It was clear that significantly (p50.05) higher drug released percentages (P 2h and P 8h ) were achieved when the cubosomes were prepared at the lower GMO: PVS ratio (10: 1) and the higher hydrotrope: (GMO -surfactant) ratio (3: 1).…”

Section: In Vitro Drug Release Studiesmentioning

confidence: 99%

Duodenum-triggered delivery of pravastatin sodium: II. Design, appraisal and pharmacokinetic assessments of enteric surface-decorated nanocubosomal dispersions

et al. 2016

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Context: Pravastatin sodium (PVS) is a freely water-soluble HMG-CoA inhibitor that suffers from instability at gastric pH, extensive first pass metabolism, short elimination half-life (1-3 h) and low oral bioavailability (18%). Objective: To overpower these drawbacks and to maximize drug absorption at its main site of absorption at the duodenum, enteric surface-coated PVS-loaded nanocubosomal dispersions were presented. Materials and methods: Glyceryl monooleate (GMO)-based dispersions were developed by the fragmentation or the liquid precursor methods using Pluronic Õ F127 or Cremophor Õ EL as surfactants. As a challenging entericcoating approach, the promising dispersions were surface-coated via lyophilization with Eudragit Õ L100-55; a duodenum-targeting polymer. The drug content, particle size, zeta potential, morphology and release studies of PVS-loaded dispersions were evaluated before and after surface-coating. Compared to an aqueous PVS solution, the pharmacokinetics of the best achieved system (E-F8) was evaluated (UPLC-MS/MS) in rats. Results: The enteric surfacecoated nanocubosomal dispersions were more or less spherical in shape and showed high drug-loading, negative zeta potential values and fine-tuned biphasic drug-release patterns characterized by retarded (2 h) and sustained (10 h) phases in pH 1.2 and pH 6.8, respectively. E-F8 system showed significantly (p50.05) higher oral bioavailability, delayed T max and prolonged MRT 0À1 following oral administration in rats. Conclusions: The duodenum-triggering potential and the controlled-release characteristics of the best achieved system for smart PVS delivery were revealed.

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“…Flow-through implant cells detected the immediate release of sunitinib from ion-370 exchange microspheres in a small vessel-like chamber, and would be best suited to discriminate between different types of drug-eluting spheres. Slow release in dialysis cylinder inserts only correlated because of drug redistribution mechanisms between tissue and plasma in vivo and was not the method of choice for fast-eluting microspheres due to low drug diffusion (Wacker, 2013;Wacker, 2014). A flow-through set-up with relatively low shear without a membrane 375 barrier might be envisaged.…”

Section: Resultsmentioning

confidence: 99%

Sunitinib-eluting beads for chemoembolization: Methods for in vitro evaluation of drug release

Fuchs

Bize

Denys

et al. 2015

International Journal of Pharmaceutics

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Drug-eluting microspheres are used for embolization of hypervascular tumors and allow for 15 local controlled drug release. Although the drug release from the microspheres relies on fast ion-exchange, so far only slow-releasing in vitro dissolution methods have been correlated to in vivo data. Three in vitro release methods are assessed in this study for their potential to predict slow in vivo release of sunitinib from chemoembolization spheres to the plasma, and fast local in vivo release obtained in an earlier study in rabbits. 20Release in an orbital shaker was slow (t 50% = 4.5 h, 84% release) compared to fast release in USP 4 flow-through implant cells (t 50% = 1 h, 100% release). Release of sunitinib from microspheres in saline in dialysis inserts was prolonged and incomplete (t 50% = 9 d, 68% release) due to low drug diffusion through the dialysis membrane. The slow-release profile fitted best to low sunitinib plasma AUC following injection of sunitinib-eluting spheres. Although limited by lack of 25 standardization, release in the orbital shaker fitted best to local in vivo sunitinib concentrations.Drug release in USP flow-through implant cells was too fast to correlate with local concentrations, although this method is preferred to discriminate between different sphere types. 3 Graphical Abstract KeywordsIn vitro drug release, sunitinib, drug-eluting beads, USP dissolution apparatus 4, 35 chemoembolization, in vitro-in vivo correlation

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Nanocarriers for intravenous injection—The long hard road to the market

Cited by 147 publications

References 126 publications

Bio-inspired artemether-loaded human serum albumin nanoparticles for effective control of malaria-infected erythrocytes

Bio-inspired artemether-loaded human serum albumin nanoparticles for effective control of malaria-infected erythrocytes

Duodenum-triggered delivery of pravastatin sodium: II. Design, appraisal and pharmacokinetic assessments of enteric surface-decorated nanocubosomal dispersions

Sunitinib-eluting beads for chemoembolization: Methods for in vitro evaluation of drug release

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