Investigation of polymeric nanoparticles as carriers of enalaprilat for oral administration

Ahlin, P; Kristl, Julijana; Kristl, Albin; Vrečer, Franc

doi:10.1016/s0378-5173(02)00076-5

Cited by 138 publications

(86 citation statements)

References 8 publications

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“…Zeta potential results (Table 2) showed that both empty and drug-loaded nanosphere formulations exhibited a negative charge with values ranging from K38.9 to K36.0 mV, typically observed for these types of systems [27]. The surface charge of colloidal particles can arise by a number of means, e.g.…”

Section: Characteristics Of Xan and 3-meoxan-loaded Nanospheresmentioning

confidence: 99%

Development and characterization of PLGA nanospheres and nanocapsules containing xanthone and 3-methoxyxanthone

Teixeira

Alonso

Pinto

et al. 2005

European Journal of Pharmaceutics and Biopharmaceutics

161

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The aim of the present work was to develop and characterize two different nanosystems, nanospheres and nanocapsules, containing either xanthone (XAN) or 3-methoxyxanthone (3-MeOXAN), with the final goal of improving the delivery of these poorly water-soluble compounds. The xanthones-loaded nanospheres (nanomatrix systems) and nanocapsules (nanoreservoir systems), made of poly(DL-lactideco-glycolide) (PLGA), were prepared by the solvent displacement technique. The following characteristics of nanoparticle formulations were determined: particle size and morphology, zeta potential, incorporation efficiency, thermal behaviour, in vitro release profiles and physical stability at 4 8C. The nanospheres had a mean diameter !170 nm, a narrow size distribution (polydispersity index !0.1), and a negative surface charge (zeta potential !K36 mV). Their incorporation efficiencies were 33% for XAN and 42% for 3-MeOXAN. The presence of the xanthones did not affect the nanospheres size and zeta potential. DSC studies indicated that XAN and 3-MeOXAN were dispersed at a molecular level within the polymeric nanomatrix. Nanocapsules were also nanometric (mean size !300 nm) and exhibited a negative charge (zeta potential !K36 mV). Their incorporation efficiency values (O77%) were higher than those corresponding to nanospheres for both xanthones. The release of 3-MeOXAN from nanocapsules was similar to that observed for the correspondent nanoemulsion, indicating that drug release is mainly governed by its partition between the oil core and the external aqueous medium. In contrast, the release of XAN from nanocapsules was significantly slower than from the nanoemulsion, a behaviour that suggests an interaction of the drug with the polymer. Nanocapsule formulations exhibited good physical stability at 4 8C during a 4-month period for XAN and during a 3-month period for 3-MeOXAN. q

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Section: Characteristics Of Xan and 3-meoxan-loaded Nanospheresmentioning

confidence: 99%

Development and characterization of PLGA nanospheres and nanocapsules containing xanthone and 3-methoxyxanthone

Teixeira

Alonso

Pinto

et al. 2005

European Journal of Pharmaceutics and Biopharmaceutics

161

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“…In case of water miscible solvent like acetone, no proper emulsion is formed even in presence of stabilizer, hence it resulted in precipitation leading to the formation of larger particles [12]. They have also reported synthesis of 250-400 nm PLGA with the use of acetone and 350-450 nm with DCM.…”

Section: Impact Of Solvent On the Particle Size Of Plgamentioning

confidence: 99%

Encapsulation of Berberine in Nano-Sized PLGA Synthesized by Emulsification Method

Khemani¹,

Sharon²,

Sharon³

2012

ISRN Nanotechnology

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Nanoparticles of PLGA (polylactide glycolic acid) were prepared using biodegradable poly (D, L-lactide-co-glycolide)-75 : 25, by emulsification method using PVA (Mol. Wt. 9000) or didodecyl dimethyl ammonium bromide (DMAB) as surfactant. Nanoparticles were morphologically characterized using scanning electron microscope (SEM) and particle size analyzer. The distribution of size of PLGA nanoparticles was in the range of 48-211 nm. Berberine, a yellow isoquinoline alkaloid that is used as traditional anticancer drug, was loaded on to PLGA nanoparticles by single emulsion as well as multiple emulsion solvent evaporation techniques. Particle size analysis showed an increase in berberine loaded PLGA NP size to 180-310 nm when PVA was used as a stabilizer. Whereas use of DMAB as a stabilizer led to precipitation. In vitro drug release analysis revealed that acidic pH of 5.5 was more suitable for release of berberine than pH 7.4.

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“…Examples are savoxepine, 84 doxorubicin, 85 irinotecan, 86 paclitaxel, 87,88 antiestrogen RU58668, 89 tyrphostin AG-1295, 90 lidocaine, 91 propranolol hydrochloride, 92 heparin, 93 and enalaprilat. 94 Basically, drug entrapment efficiency depends on the solid-state drug solubility in PLA/PLGA polymer (solid dissolution or dispersion), which is related to the polymer composition (lactic/glycolic ratio), the molecular weight, the drugpolymer interaction and the presence of end-functional groups (ester or carboxyl). [95][96][97][98][99] The PEG moiety has no or little effect on drug loading.…”

Section: Drug Loadingmentioning

confidence: 99%

“…Drug entrapment efficiency can reach more than 80% 84,92,91 and drug content up to 50%. 91 In most cases, however, drug contents are 5-10% (wt/wt) of nanoparticle weights 86,88,94,96,97,102 or even less. 87 Therefore, when formulating drug nanoparticles, it should always be kept in mind that generally as high as 90% of the material to be administered will likely be nanoparticle excipients with their potential toxicity.…”

Section: Drug Loadingmentioning

confidence: 99%

Drug transport to brain with targeted nanoparticles

2005

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Summary: Nanoparticle drug carriers consist of solid biodegradable particles in size ranging from 10 to 1000 nm (50 -300 nm generally). They cannot freely diffuse through the bloodbrain barrier (BBB) and require receptor-mediated transport through brain capillary endothelium to deliver their content into the brain parenchyma. Polysorbate 80-coated polybutylcyanoacrylate nanoparticles can deliver drugs to the brain by a still debated mechanism. Despite interesting results these nanoparticles have limitations, discussed in this review, that may preclude, or at least limit, their potential clinical applications. Long-circulating nanoparticles made of methoxypoly(ethylene glycol)-polylactide or poly(lactide-co-glycolide) (mPEG-PLA/ PLGA) have a good safety profiles and provide drug-sustained release. The availability of functionalized PEG-PLA permits to prepare target-specific nanoparticles by conjugation of cell surface ligand. Using peptidomimetic antibodies to BBB transcytosis receptor, brain-targeted pegylated immunonanoparticles can now be synthesized that should make possible the delivery of entrapped actives into the brain parenchyma without inducing BBB permeability alteration. This review presents their general properties (structure, loading capacity, pharmacokinetics) and currently available methods for immunonanoparticle preparation.

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Investigation of polymeric nanoparticles as carriers of enalaprilat for oral administration

Cited by 138 publications

References 8 publications

Development and characterization of PLGA nanospheres and nanocapsules containing xanthone and 3-methoxyxanthone

Development and characterization of PLGA nanospheres and nanocapsules containing xanthone and 3-methoxyxanthone

Encapsulation of Berberine in Nano-Sized PLGA Synthesized by Emulsification Method

Drug transport to brain with targeted nanoparticles

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