Synergistic effect of magnesium stearate and fine lactose in improving aerosolization performance of fluticasone propionate in dry powder formulation.

Autor: He X; School of Pharmacy, Shenyang Key Laboratory of Intelligent Mucosal Drug Delivery Systems, Shenyang Pharmaceutical University, Shenyang 110016, China., Li J; School of Pharmacy, Shenyang Key Laboratory of Intelligent Mucosal Drug Delivery Systems, Shenyang Pharmaceutical University, Shenyang 110016, China., Wen X; School of Pharmacy, Shenyang Key Laboratory of Intelligent Mucosal Drug Delivery Systems, Shenyang Pharmaceutical University, Shenyang 110016, China., Ma S; School of Pharmacy, Shenyang Key Laboratory of Intelligent Mucosal Drug Delivery Systems, Shenyang Pharmaceutical University, Shenyang 110016, China., An Y; School of Pharmacy, Shenyang Key Laboratory of Intelligent Mucosal Drug Delivery Systems, Shenyang Pharmaceutical University, Shenyang 110016, China., Zhang X; School of Pharmacy, Shenyang Key Laboratory of Intelligent Mucosal Drug Delivery Systems, Shenyang Pharmaceutical University, Shenyang 110016, China; Joint International Research Laboratory of Intelligent Drug Delivery Systems, Ministry of Education, China., Guan J; School of Pharmacy, Shenyang Key Laboratory of Intelligent Mucosal Drug Delivery Systems, Shenyang Pharmaceutical University, Shenyang 110016, China; Joint International Research Laboratory of Intelligent Drug Delivery Systems, Ministry of Education, China., Mao S; School of Pharmacy, Shenyang Key Laboratory of Intelligent Mucosal Drug Delivery Systems, Shenyang Pharmaceutical University, Shenyang 110016, China; Joint International Research Laboratory of Intelligent Drug Delivery Systems, Ministry of Education, China. Electronic address: maoshirui@syphu.edu.cn.
Jazyk: angličtina
Zdroj: International journal of pharmaceutics [Int J Pharm] 2024 Oct 25; Vol. 664, pp. 124609. Date of Electronic Publication: 2024 Aug 18.
DOI: 10.1016/j.ijpharm.2024.124609
Abstrakt: Magnesium stearate (MgSt) and lactose fines are often used as ternary components in carrier-based dry powder inhalers (DPIs) to improve fine particle fraction (FPF), but whether they act synergistically to improve aerosolization performance of DPI formulations is currently less studied. In addition, the applicability of utilizing powder rheological parameters to predict the FPF needs to be further verified. Thus, in this study, using fluticasone propionate (FP) as a model drug, effect of lactose fines addition in 0.5% MgSt containing DPI formulations on their powder and aerodynamic properties was explored. Influence of MgSt and fines mixing order on the DPIs performance was also investigated. The results showed that addition of lactose fines (1-10%) in 0.5% MgSt containing formulations could further improve flowability and enhance adhesion of the mixtures, and they could act synergistically to improve FPF. Moreover, the presence of 0.5% MgSt can greatly reduce the amount of lactose fines required to achieve the comparable FPF. The mixing order can affect distribution of MgSt on the carrier surface, with higher FPF noted when MgSt was mixed with carrier first, followed by lactose fines. A good linear relationship between powder rheological parameters such as basic flowability energy (BFE), Permeability and FPF was disclosed. In conclusion, in FP based DPIs, MgSt and lactose fines act synergistically to enhance FPF by tuning powder characteristics. Good flowability (27.39%) and strong adhesion (72.61%) contributed to the enhanced drug deposition in the lung.
Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
(Copyright © 2024. Published by Elsevier B.V.)
Databáze: MEDLINE
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