Spray-dried didanosine-loaded polymeric particles for enhanced oral bioavailability

Seremeta, Katia Pamela; Tur, María Isabel Reyes; Pérez, Sandra Martínez; Höcht, Christián; Taira, Carlos A.; Hernández, Orestes Darío López; Sosnik, Alejandro

doi:10.1016/j.colsurfb.2014.09.055

Cited by 17 publications

(8 citation statements)

References 63 publications

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“…Moreover, although during the drying A C C E P T E D M A N U S C R I P T ACCEPTED MANUSCRIPT 7 process, the droplets could be exposed to high temperature, this exposure time is extremely short (in the range of milliseconds or seconds) [18,35,50]. Under these conditions, drug degradation is not anticipated [51]. The spray-drying technique was conceived as a dehydration process used to prolong the lifespan of the product.…”

Section: Main Advantages Of the Spray-drying Processmentioning

confidence: 99%

“…Drug-loaded MPs were spherical with average diameter between 36 and 118 μm (Figure 9) and yield between 37.7% and 64.9%. Oral administration of the optimized formulation to rats resulted in a statistically significant 2.5-fold increase of the drug bioavailability with respect to a didanosine aqueous solution(Figure 9C)[51]. Spraydrying enables the encapsulation of active agents of diverse physicochemical properties polymer matrices (synthetic, semi-synthetic or natural origin) under very mild and non-detrimental conditions and with high encapsulation efficiency (%EE) and…”

mentioning

confidence: 97%

“…For example, Seremeta et al encapsulated the anti-HIV didanosine within poly(epsilon-caprolactone) (PCL) MPs both by suspension and simple emulsion followed for spray-drying to avoid its fast gastric degradation that leads to low oral bioavailability (20-40%)[51]. The device used in this study was a Mini Spray Dryer B-191.…”

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confidence: 98%

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Advantages and challenges of the spray-drying technology for the production of pure drug particles and drug-loaded polymeric carriers

Sosnik

Seremeta

2015

Advances in Colloid and Interface Science

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Section: Main Advantages Of the Spray-drying Processmentioning

confidence: 99%

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confidence: 97%

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Advantages and challenges of the spray-drying technology for the production of pure drug particles and drug-loaded polymeric carriers

Sosnik

Seremeta

2015

Advances in Colloid and Interface Science

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486

252

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“…[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. [21] In addition, the solid particles obtained by this method have higher chemical and physical stability. 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.…”

Section: Introductionmentioning

confidence: 97%

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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“…Didanosine is an antiretroviral drug used for HIV (Human Immunodeficiency Virus) treatment (Seremeta et al, 2014) and its solubility data are scarce in the literature, especially considering physiologic conditions, which may hamper the biopharmaceutic classification.…”

Section: Introductionmentioning

confidence: 99%

Solubility evaluation of didanosine: a comparison between the equilibrium method and intrinsic dissolution for biopharmaceutics classification purposes

Dezani

Ferreira

et al. 2017

Braz. J. Pharm. Sci.

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BCS (Biopharmaceutics Classification System) and BDDCS (Biopharmaceutics Drug DispositionClassification System) were proposed as tools for classifying drugs into four categories. Both systems consider the solubility as an important characteristic for the classification of compounds in drug development and in vivo disposition prediction. Although some results of drug solubility can be found in the literature, the aforementioned characteristic is not entirely clear when considering didanosine (ddI). Based on that, the solubility of ddI was evaluated using equilibrium and intrinsic dissolution methods. For the equilibrium method, excess amount of ddI was added to each media until obtaining a supersaturated solution and the mixture was submitted to agitation at 37 °C. For the intrinsic dissolution method, the drug was compressed into the Wood's apparatus matrix and subjected to dissolution in each media with agitation at 37 °C. The results obtained from the equilibrium method indicated that it was necessary 139.37 mL of pH 1.2 media, 87.72 mL of pH 4.5 media, 12.54 mL of pH 6.8 media, 5.03 mL of pH 7.5 media and 7.65 mL of purified water for drug solubilization. Furthermore, a very fast intrinsic dissolution rate (IDR) was obtained for each media: 0.1 mg/min/cm² (pH 1.2), 0.2 mg/min/cm² (pH 4.5), 0.2 mg/ min/cm² (pH 6.8), 0.1 mg/min/cm² (pH 7.5) and 0.1 mg/min/cm² (purified water). Based on these results, ddI can be considered as a highly soluble drug for both equilibrium and intrinsic dissolution methods.

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Spray-dried didanosine-loaded polymeric particles for enhanced oral bioavailability

Cited by 17 publications

References 63 publications

Advantages and challenges of the spray-drying technology for the production of pure drug particles and drug-loaded polymeric carriers

Advantages and challenges of the spray-drying technology for the production of pure drug particles and drug-loaded polymeric carriers

Novel spray-dried PHA microparticles for antitumor drug release

Solubility evaluation of didanosine: a comparison between the equilibrium method and intrinsic dissolution for biopharmaceutics classification purposes

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