Spray-dried solid inhalable N-acetylcysteine microparticles:
Preparation and mucolytic activity testing

J 2025

Spray-dried solid inhalable N-acetylcysteine microparticles: Preparation and mucolytic activity testing

HOŘAVOVÁ, Hana; Andrea HORKÁ; Sylvie PAVLOKOVÁ; Jana KÁNSKÁ; František LÍZAL et al.

Základní údaje

Originální název

Spray-dried solid inhalable N-acetylcysteine microparticles: Preparation and mucolytic activity testing

Autoři

HOŘAVOVÁ, Hana ; Andrea HORKÁ ; Sylvie PAVLOKOVÁ ; Jana KÁNSKÁ; František LÍZAL a Jan GAJDZIOK

Vydání

JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY, Amsterdam, ELSEVIER, 2025, 1773-2247

Další údaje

Jazyk

angličtina

Typ výsledku

Článek v odborném periodiku

Obor

30104 Pharmacology and pharmacy

Stát vydavatele

Nizozemské království

Utajení

není předmětem státního či obchodního tajemství

Odkazy

URL

Impakt faktor

Impact factor: 4.900 v roce 2024

Označené pro přenos do RIV

Ano

Kód RIV

RIV/00216224:14160/25:00142980

Organizační jednotka

Farmaceutická fakulta

Klíčová slova anglicky

Spray drying; N-acetylcysteine; Microparticles; Dry powders; Pulmonary drug delivery

Štítky

rivok, ÚFT

Příznaky

Mezinárodní význam, Recenzováno

Změněno: 12. 3. 2026 22:12, Mgr. Irena Doubková

Anotace

V originále

Inhalation is the preferred administration for treating pulmonary disorders like cystic fibrosis, with the use of mucolytics such as N-acetylcysteine being the main therapeutic strategy. This study aimed to develop spray-dried inhalable microparticles, using N-acetylcysteine and mannitol as a carrier and osmotic agent. Various methodologies were assessed to optimize the spray drying process, including different drying conditions and additives in the dispersion. The results demonstrated the requirements for particular excipients to formulate N-acetylcysteine–mannitol inhalable microparticles by spray drying. Incorporating a neutralizing agent (sodium hydroxide) or glass transition temperature modifiers (dextran, maltodextrin, chitosan) produced spherical primary particles that readily agglomerated into large clusters. Leucine, as an antiadherent agent, demonstrated efficacy as the sole excipient at a concentration of 20–25 %, facilitating the formulation of particles with appropriate size, shape, and morphology. Inhalable particles (mass median aerodynamic diameter 5.95 ± 1.53 μm, fine particle fraction 33.06 %) were prepared by modifying process parameters (nozzle size reduction, feed solution dilution). The encapsulated N-acetylcysteine also showed sustained mucolytic activity in vitro (35.3 % viscosity reduction after 120 min), using an innovative method. This work represents the complex study of N-acetylcysteine inhalable microparticles preparation as a possible approach to overcome liquid formulation.

Návaznosti

MUNI/A/1213/2020, interní kód MU

Název: Formulace a hodnocení depozice mikročásticových systémů k aplikaci do plic. (Akronym: plicní mikročástice)

Investor: Masarykova univerzita, Formulace a hodnocení depozice mikročásticových systémů k aplikaci do plic.

Citovat

HOŘAVOVÁ, Hana; Andrea HORKÁ; Sylvie PAVLOKOVÁ; Jana KÁNSKÁ; František LÍZAL a Jan GAJDZIOK. Spray-dried solid inhalable N-acetylcysteine microparticles: Preparation and mucolytic activity testing. JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY. Amsterdam: ELSEVIER, 2025, roč. 114, B, s. 1-14. ISSN 1773-2247. Dostupné z: https://doi.org/10.1016/j.jddst.2025.107622.

@article{2541717,
   author = {Hořavová, Hana and Horká, Andrea and Pavloková, Sylvie and Kánská, Jana and Lízal, František and Gajdziok, Jan},
   article_location = {Amsterdam},
   article_number = {B},
   doi = {https://doi.org/10.1016/j.jddst.2025.107622},
   keywords = {Spray drying; N-acetylcysteine; Microparticles; Dry powders; Pulmonary drug delivery},
   language = {eng},
   issn = {1773-2247},
   journal = {JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY},
   title = {Spray-dried solid inhalable N-acetylcysteine microparticles: Preparation and mucolytic activity testing},
   url = {https://doi.org/10.1016/j.jddst.2025.107622},
   volume = {114},
   year = {2025}
}

TY  - JOUR
ID  - 2541717
AU  - Hořavová, Hana - Horká, Andrea - Pavloková, Sylvie - Kánská, Jana - Lízal, František - Gajdziok, Jan
PY  - 2025
TI  - Spray-dried solid inhalable N-acetylcysteine microparticles: Preparation and mucolytic activity testing
JF  - JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
VL  - 114
IS  - B
SP  - 1-14
EP  - 1-14
PB  - ELSEVIER
SN  - 17732247
KW  - Spray drying
KW  - N-acetylcysteine
KW  - Microparticles
KW  - Dry powders
KW  - Pulmonary drug delivery
UR  - https://doi.org/10.1016/j.jddst.2025.107622
N2  - Inhalation is the preferred administration for treating pulmonary disorders like cystic fibrosis, with the use of mucolytics such as N-acetylcysteine being the main therapeutic strategy. This study aimed to develop spray-dried inhalable microparticles, using N-acetylcysteine and mannitol as a carrier and osmotic agent. Various methodologies were assessed to optimize the spray drying process, including different drying conditions and additives in the dispersion. The results demonstrated the requirements for particular excipients to formulate N-acetylcysteine–mannitol inhalable microparticles by spray drying. Incorporating a neutralizing agent (sodium hydroxide) or glass transition temperature modifiers (dextran, maltodextrin, chitosan) produced spherical primary particles that readily agglomerated into large clusters. Leucine, as an antiadherent agent, demonstrated efficacy as the sole excipient at a concentration of 20–25 %, facilitating the formulation of particles with appropriate size, shape, and morphology. Inhalable particles (mass median aerodynamic diameter 5.95 ± 1.53 μm, fine particle fraction 33.06 %) were prepared by modifying process parameters (nozzle size reduction, feed solution dilution). The encapsulated N-acetylcysteine also showed sustained mucolytic activity in vitro (35.3 % viscosity reduction after 120 min), using an innovative method. This work represents the complex study of N-acetylcysteine inhalable microparticles preparation as a possible approach to overcome liquid formulation.
ER  -

HOŘAVOVÁ, Hana; Andrea HORKÁ; Sylvie PAVLOKOVÁ; Jana KÁNSKÁ; František LÍZAL a Jan GAJDZIOK. Spray-dried solid inhalable N-acetylcysteine microparticles: Preparation and mucolytic activity testing. \textit{JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY}. Amsterdam: ELSEVIER, 2025, roč.~114, B, s.~1-14. ISSN~1773-2247. Dostupné z: https://doi.org/10.1016/j.jddst.2025.107622.

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