Biodegradable polymeric microparticles for drug delivery and vaccine formulation: the surface attachment of hydrophilic species using the concept of poly(ethylene glycol) anchoring segments

Coombes, Allan G.A.; Tasker, S.; Lindblad, Marianne; Holmgren, Jan; Hoste, Katty; Toncheva, Veska; Schacht, Etienne; Davies, Martyn C.; Illum, Lisbeth; Davis, S.S.

doi:10.1016/s0142-9612(97)00051-3

Cited by 79 publications

(47 citation statements)

References 35 publications

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“…All values for mass median aerodynamic diameter, emitted dose, fine particle fraction, percent of drug remaining in the nebulizer, and percent of drug deposited in the induction port of the BUD-SSMs were significantly superior compared with Pulmicort Respules ® due to the particle size and presence of the hydrophilic polymer (PEG) in the outer shell of the SSMs, which induced a repulsive steric interaction between the particles that could effectively decrease the overall adhesive forces, thereby allowing more efficient aerosolization and stabilizing the colloidal suspension in air. 29,61,62 The geometric standard deviation values of BUD-SSMs were significantly (P , 0.05) higher than those of the Pulmicort Respules ® due to the effect of operating the cascade impactor at ambient temperature, which affected smaller droplets more than the larger droplets generated by the nebulizer, and produced a wider spread of geometric standard deviation values, as previously reported. 63 The improved aerodynamic performance of the BUD-SSMs leads to a decrease in the therapeutic dose and a reduction in systemic side effects.…”

Section: Aerodynamic Characterizationsupporting

confidence: 75%

Rehydrated sterically stabilized phospholipid nanomicelles of budesonide for nebulization: physicochemical characterization and in vitro, in vivo evaluations

Sahib¹,

Darwis²,

Peh³

et al. 2011

IJN

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Background: Inhaled corticosteroids provide unique systems for local treatment of asthma or chronic obstructive pulmonary disease. However, the use of poorly soluble drugs for nebulization has been inadequate, and many patients rely on large doses to achieve optimal control of their disease. Theoretically, nanotechnology with a sustained-release formulation may provide a favorable therapeutic index. The aim of this study was to determine the feasibility of using sterically stabilized phospholipid nanomicelles of budesonide for pulmonary delivery via nebulization. Methods: PEG 5000 -DSPE polymeric micelles containing budesonide (BUD-SSMs) were prepared by the coprecipitation and reconstitution method, and the physicochemical and pharmacodynamic characteristics of BUD-SSMs were investigated. Results: The optimal concentration of solubilized budesonide at 5 mM PEG 5000 -DSPE was 605.71 ± 6.38 µg/mL, with a single-sized peak population determined by photon correlation spectroscopy and a particle size distribution of 21.51 ± 1.5 nm. The zeta potential of BUD-SSMs was −28.43 ± 1.98 mV. The percent entrapment efficiency, percent yield, and percent drug loading of the lyophilized formulations were 100.13% ± 1.09%, 97.98% ± 1.95%, and 2.01% ± 0.02%, respectively. Budesonide was found to be amorphous by differential scanning calorimetry, and had no chemical interaction with PEGylated polymer according to Fourier transform infrared spectroscopy. Transmission electron microscopic images of BUD-SSMs revealed spherical nanoparticles. BUD-SSMs exhibited prolonged dissolution behavior compared with Pulmicort Respules ® (P , 0.05). Aerodynamic characteristics indicated significantly higher deposition in the lungs compared with Pulmicort Respules ® . The mass median aerodynamic, geometric standard deviation, percent emitted dose, and the fine particle fraction were 2.83 ± 0.08 µm, 2.33 ± 0.04 µm, 59.13% ± 0.19%, and 52.31% ± 0.25%, respectively. Intratracheal administration of BUD-SSMs 23 hours before challenge (1 mg/kg) in an asthmatic/chronic obstructive pulmonary disease rat model led to a significant reduction in inflammatory cell counts (76.94 ± 5.11) in bronchoalveolar lavage fluid compared with administration of Pulmicort Respules ® (25.06 ± 6.91). Conclusion:The BUD-SSMs system might be advantageous for asthma or chronic obstructive pulmonary disease and other inflammatory airway diseases.

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Section: Aerodynamic Characterizationsupporting

confidence: 75%

Rehydrated sterically stabilized phospholipid nanomicelles of budesonide for nebulization: physicochemical characterization and in vitro, in vivo evaluations

Sahib¹,

Darwis²,

Peh³

et al. 2011

IJN

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“…As can be seen, the plateau is obtained for DexP 15 concentrations above 1 g/L (corresponding to [DexP]/ S = 0.013g/L/m 2 ) and the ⌫ max value is 6.6 mg/m 2 . It should be noted that ⌫ max is smaller than the ⌫ values determined for NS em prepared at DexP 15 concentrations higher than 2.5 g/L.…”

Section: Resultsmentioning

confidence: 85%

“…In this case, the POE segments provide the anchor to the particle shell while the hydrophilic dextran chains are protruding into the solution. 15 In previous papers, 16,17 we showed that the attachment of phenoxy groups on dextran leads to derivatives (DexP) whose amphiphilic properties clearly are evidenced by fluorescence and viscosity measurements. These derivatives adsorb onto hydrophobic polystyrene surfaces through their hydrophobic sites.…”

Section: Introductionmentioning

confidence: 96%

Surface modification of poly(lactic acid) nanospheres using hydrophobically modified dextrans as stabilizers in an o/w emulsion/evaporation technique

Rouzes

Gref

Léonard

et al. 2000

J. Biomed. Mater. Res.

106

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Sterically stabilized biocompatible poly(lactic acid) (PLA) nanospheres were prepared by an o/w emulsion/evaporation technique, using hydrophobically modified dextrans (DexP) as the emulsion stabilizer. Photon correlation spectroscopy, zetametry, and differential scanning calorimetry studies corroborated that interfacial adhesion between immiscible dextran and PLA chains was achieved by compatibilization of polymer segments via hydrophobic groups grafted onto dextran and thus leading to the formation of entanglements between the hydrophobic dextran parts and the PLA matrix. The presence of dextran exposed at the particle surface was confirmed by X-ray photoelectron spectroscopy and by the fact that the suspensions showed an increased stability in concentrated NaCl solutions and a reduction of bovine serum albumin adsorption compared to uncoated PLA nanoparticles. A comparison of the characteristics of PLA nanospheres DexP-coated via the emulsion procedure (NS(em)) with those of PLA particles coated by DexP adsorption (NS(ad)) suggests that the conformation of the polymer in the superficial layers may be different. However, both DexP layers behave similarly in terms of stability and protein adsorption.

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“…There is growing interest and investment in the use of polymer-based systems in drug discovery and product development to effectively overcome problems related to stability and bioavailability [1,2]. Microparticulate carrier systems made from naturally occurring biodegradable and bioadhesive (mucoadhesive) polymers have attracted considerable attention over the years [3].…”

Section: Introductionmentioning

confidence: 99%

Formulation and Evaluation of Glutaraldehyde-Crosslinked Chitosan Microparticles for the Delivery of Ibuprofen

Ofokansi¹,

Kenechukwu²,

Isah³

et al. 2013

Trop. J. Pharm Res

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Biodegradable polymeric microparticles for drug delivery and vaccine formulation: the surface attachment of hydrophilic species using the concept of poly(ethylene glycol) anchoring segments

Cited by 79 publications

References 35 publications

Rehydrated sterically stabilized phospholipid nanomicelles of budesonide for nebulization: physicochemical characterization and in vitro, in vivo evaluations

Rehydrated sterically stabilized phospholipid nanomicelles of budesonide for nebulization: physicochemical characterization and in vitro, in vivo evaluations

Surface modification of poly(lactic acid) nanospheres using hydrophobically modified dextrans as stabilizers in an o/w emulsion/evaporation technique

Formulation and Evaluation of Glutaraldehyde-Crosslinked Chitosan Microparticles for the Delivery of Ibuprofen

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