Critical Solvent Properties Affecting the Particle Formation Process and Characteristics of Celecoxib-Loaded PLGA Microparticles via Spray-Drying

Wan, Feng; Bohr, Adam; Maltesen, Morten Jonas; Bjerregaard, Simon; Yang, Mingshi

doi:10.1007/s11095-012-0943-x

Cited by 61 publications

(38 citation statements)

References 37 publications

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“…As a general observation, it might be said that the thermal and magnetic properties together with biocompatibility or biodegradability properties might allow for their use in several of the proposed biomedical applications, thus avoiding the problem of unexpected and unpredictable physical changes that can happen when they are processed during their production (such as thermal stability changes due to PLGA solubilization/lyophilization or iron oxide interaction), when applied to the human body, or when they are stored for later use. Several studies have demonstrated the importance of thermal characterization of bulk PLGA and materials based on such polymer, for better understanding of its stabilities, degradation, among other properties [20][21][22] . In this work, hollow PLGA nanospheres and PLGA magnetic nanospheres (with maghemite entrapment) were characterized.…”

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confidence: 99%

Study of Thermal Degradation of PLGA, PLGA Nanospheres and PLGA/Maghemite Superparamagnetic Nanospheres

et al. 2015

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Poly(glycolide-co-lactide) (PLGA) nanospheres containing magnetic materials have been extensively studied because of its biomedical applications. Therefore, it is very important to know thermal properties of these materials in addition to other physical properties. Thermal degradation activation energy (E α ) of PLGA nanospheres with maghemite entrapment (PLGA-Mag), PLGA nanospheres (hollow spheres) (PLGA-H) obtained by an emulsion method and unprocessed PLGA (PLGA-R) were calculated by isoconversional Vyazovkin method based on data of TG analysis in order to evaluate modifications in thermal behavior caused by nanospheres obtainment process or by maghemite entrapment. Both hydrodynamic diameter in the range of 200-250 nm and polydispersity index lower than 0.3 are considered satisfactory. Thermal degradation of PLGA-R begins at higher temperatures than those of PLGA-H and PLGA-Mag, but processed samples presented increase in thermal stability, which was greater before processing by emulsion and in the presence of the magnetic materials. PLGA-Mag presents superparamagnetic behavior at room temperature.

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confidence: 99%

Study of Thermal Degradation of PLGA, PLGA Nanospheres and PLGA/Maghemite Superparamagnetic Nanospheres

et al. 2015

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“…Particle size was measured using the scanning electron microscopy images (as described above) with the help of ImageJ software (37, 38). Martin’s diameter of ~150 randomly selected particles was determined in a fixed downwards direction from three different SEM images and D 10 , D 50 and D 90 were calculated from the size distribution data.…”

Section: Methodsmentioning

confidence: 99%

Understanding the Impacts of Surface Compositions on the In-Vitro Dissolution and Aerosolization of Co-Spray-Dried Composite Powder Formulations for Inhalation

Mangal

Park

et al. 2018

Pharm Res

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Purpose: Dissolution behavior of dry powder inhaler (DPI) antibiotic formulations in the airways may affect their efficacy especially for poorly-soluble antibiotics such as azithromycin. The main objective of this study was to understand the effects of surface composition on the dissolution of spray dried azithromycin powders by itself and in combination with colistin. Methods: Composite formulations of azithromycin (a poorly water-soluble molecule) and colistin (a water-soluble molecule) were produced by spray drying. The resultant formulations were characterized for particle size, morphology, surface composition, solid-state properties, solubility and dissolution. Results: The results demonstrate that surfaces composition has critical impacts on the dissolution of composite formulations. Colistin was shown to increase the solubility of azithromycin. For composite formulations with no surface colistin, azithromycin released at a similar dissolution rate as the spray-dried azithromycin alone. An increase in surface colistin concentration was shown to accelerate the dissolution of azithromycin. The dissolution of colistin from the composite formulations was significantly slower than the spray-dried pure colistin. In addition, FTIR spectrum showed intermolecular interactions between azithromycin and colistin in the composite formulations, which could contribute to the enhanced solubility and dissolution of azithromycin. Conclusions: Our study provides fundamental understanding of the effects of surface concentration of colistin on azithromycin dissolution of co-spray-dried composite powder formulations.

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“…The reason is that these solvents evaporate at a temperature lower than the melting point and the glass transition temperature of the most of the other hydrophobic polymers. [13,[15][16] Well-known, spray-drying was considered as dewatering process, however, it is also possible to encapsulate hydrophilic and hydrophobic active compounds in various formulations. [17][18][19] One of the interesting facts of spray-drying is that the droplets are exposed to temperatures for milliseconds or seconds [15,20] , which protects active compounds from thermal degradation.…”

Section: Introductionmentioning

confidence: 99%

“…Moreover this method allows obtaining particles with the higher values of encapsulation efficiency, in contrast to the emulsion method, in which the drug separates between phases in the emulsion and, as a consequence, leads to decrease encapsulation efficiency. [22][23] The perusal of scientific studies report that the use of biopolymeric microparticles containing antitumor drugs 5-fluorouracil and paclitaxel, non-steroidal anti-inflammatory drug celecoxib, as well as antibiotics, antiviral drugs can be achieved by the spray-drying method [16,[24][25][26][27][28][29] . Recently, dosage forms of poorly soluble, toxic, short half-life drugs were obtained using the spray-drying method for treatment of lung cancer [30][31] , bronchial asthma [32] , hypertension [18] , etc.…”

Section: Introductionmentioning

confidence: 99%

Novel spray-dried PHA microparticles for antitumor drug release

et al. 2017

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The production of poly-3-hydroxybutyrate and poly-3-hydroxybutyrate/polyethylene glycol-based microparticles, loaded with antitumor drugs Paclitaxel (PTX) and 5-Fluorouracil (5-FU) by spray-drying technique was investigated. The average diameter of microparticles was found to be 3.4 ± 0.5 µm and zeta potential was about-44 mV. The addition of surfactant (PEG) did not show any effect on the morphological characteristics of the particles. But the chemical structure of drug influenced on the properties. Microparticles had heterogeneous pores on the surface when the hydrophobic PTX was encapsulated. For 5-FU loading microparticles, were established that the addition of surfactant positively influenced on the properties of particles and led to the loading of drug directly into the matrix. This is confirmed by the results of electron microscopy and dynamics of drug release in vitro. As a whole, the release profiles of PTX and 5-FU from composite P3HB/PEG-microparticles were less than from P3HBmicroparticles. The results of the morphological evaluation of Hela cells demonstrated that the use of cytostatic drugs loaded in P3HB microparticles induces morphological changes associated with apoptosis (chromatin condensation, core fragmentation, margination of nucleus). Thus, the obtained results can serve as the basis for the development of new antitumor drugs of prolonged action, intended for various modes of administration.

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Critical Solvent Properties Affecting the Particle Formation Process and Characteristics of Celecoxib-Loaded PLGA Microparticles via Spray-Drying

Cited by 61 publications

References 37 publications

Study of Thermal Degradation of PLGA, PLGA Nanospheres and PLGA/Maghemite Superparamagnetic Nanospheres

Study of Thermal Degradation of PLGA, PLGA Nanospheres and PLGA/Maghemite Superparamagnetic Nanospheres

Understanding the Impacts of Surface Compositions on the In-Vitro Dissolution and Aerosolization of Co-Spray-Dried Composite Powder Formulations for Inhalation

Novel spray-dried PHA microparticles for antitumor drug release

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