Supercritical fluid fabrication of components for a sustained-release injectable risperidone dose form

Баграташвили, В. Н.; Bogorodskii, S. E.; Egorov, A. M.; Кротова, Л. И.; Попов, В. К.; Sevast'yanov, V. I.

doi:10.1134/s1990793116070022

Cited by 5 publications

(1 citation statement)

References 14 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The entire process can be carried out at near ambient temperature (critical temperature and critical pressure for CO 2 are T cr = 31.1 • C and P cr = 7.4 MPa, respectively) providing no solvent residues in the final product. This technique is applicable to a wide range of API, e.g., wound healing peptides, antibiotics, non-steroid analgesics, and antipsychotic drugs [21][22][23]. The unambiguous advantages of this methodology include the absence of organic solvents used over all fabrication steps and the possibility to control the API release characteristics by delicately tuning the process parameters [24].…”

Section: Introductionmentioning

confidence: 99%

PLGA Carriers for Controlled Release of Levofloxacin in Anti-Tuberculosis Therapy

et al. 2022

View full text Add to dashboard Cite

Levofloxacin (LFX) is a highly effective anti-tuberculosis drug with a pronounced bactericidal activity against Mycobacterium tuberculosis (Mtb). In this work, an “organic solvent-free” approach has been used for the development of polylactic-co-glycolic acid (PLGA) microparticles and scaffolds containing LFX at a therapeutically significant concentration, providing for its sustained release. To achieve the target, both nonpolar supercritical carbon dioxide and polar supercritical trifluoromethane have been used. By changing the composition, surface morphology, size, and internal structure of the polymer carriers, one can control the kinetics of the LFX release into phosphate buffered saline solutions and physiological media, providing for its acceptable burst and desirable concentration in the prolonged phase. The biocompatibility and bactericidal efficacy of PLGA/LFX carriers assessed both in vitro (against Mtb phagocytosed by macrophages) and in vivo (against inbred BALB/c mice aerogenically infected with Mtb) demonstrated their anti-tuberculosis activity comparable with that of the standard daily intragastric levofloxacin administration. These results make it possible to consider the developed compositions as a promising candidate for anti-tuberculosis control release formulations providing for the further evaluation of their activity against Mtb and their metabolism in vivo over long periods of tuberculosis infection.

show abstract

Section: Introductionmentioning

confidence: 99%

PLGA Carriers for Controlled Release of Levofloxacin in Anti-Tuberculosis Therapy

et al. 2022

View full text Add to dashboard Cite

show abstract

A method to slow down the ionization-dependent release of risperidone loaded in a thermoresponsive poly(N-acryloyl glycinamide) hydrogel

Boustta

Vert

2017

Drug Deliv. and Transl. Res.

View full text Add to dashboard Cite

Poly(N-acryloyl glycinamide) polymers are soluble in hot aqueous media that gel rapidly on cooling. This gelatin-like behavior was previously compared with drug delivery requirements. Slow releases were demonstrated in vitro using different model molecules and macromolecules and in vivo using methylene blue. Risperidone is a weak basic drug sparingly soluble in water frequently used to treat patients suffering of schizophrenia. A standard risperidone-poly(N-acryloyl glycinamide) hydrogel formulation was selected from which the drug was allowed to release comparatively in buffered and non-buffered isotonic media at 37 °C under pseudo sink conditions. Linear release was observed in pH = 7.4 phosphate buffer whereas in buffer-free 0.15 M NaCl, the release was initially faster than in the buffer but became rapidly slower as the pH increased from 6.8 to 8.2. These features were related to the ionization-dependent solubility of risperidone. In order to minimize the ionization and thus the solubility of the drug inside the hydrogel despite outside buffering at 7.4, Mg(OH), a sparingly soluble mineral base, was added to the standard formulation. This addition resulted in a c.a. threefold increase of the zero-order release duration. The method should be applicable to other sparingly soluble weakly basic drugs.

show abstract

Physicochemical Properties of the Inclusion Complex of Moxifloxacin with Hydroxypropyl-β-Cyclodextrin Synthesized by RESS

Sukhoverkov

Le-Deygen

Egorov

et al. 2018

Russ. J. Phys. Chem. B

View full text Add to dashboard Cite

Supercritical fluid fabrication of components for a sustained-release injectable risperidone dose form

Cited by 5 publications

References 14 publications

PLGA Carriers for Controlled Release of Levofloxacin in Anti-Tuberculosis Therapy

PLGA Carriers for Controlled Release of Levofloxacin in Anti-Tuberculosis Therapy

A method to slow down the ionization-dependent release of risperidone loaded in a thermoresponsive poly(N-acryloyl glycinamide) hydrogel

Physicochemical Properties of the Inclusion Complex of Moxifloxacin with Hydroxypropyl-β-Cyclodextrin Synthesized by RESS

Contact Info

Product

Resources

About