Development of Liposomal Salbutamol Sulfate Dry Powder Inhaler Formulation

Abstract

The purpose of our study was to develop a formulation of liposomal salbutamol sulfate (SBS) dry powder inhaler (DPI) for the treatment of asthma. Liposomes of high encapsulation efficiency (more than 80%) were prepared by a vesicular phospholipid gel (VPG) technique. SBS VPG liposomes were subjected to lyophilization using different kinds of cryoprotectants in various mass ratios. Coarse lactose (63-106 m mm) in different mass ratios was used as a carrier. Magnesium stearate (0.5%) was added as a lubricator. The dry liposomal powders were then crushed by ball milling and sieved through a 400-mesh sieve to control the mean particle size at about 10 m mm. The effects of different kinds of cryoprotectants and the amount of lactose carrier on the fine particle fraction (FPF) of SBS were investigated. The results showed that the developed formulation of liposomal dry powder inhaler was obtained using lactose as a cryoprotectant with a mass ratio of lyophilized powder to carrier lactose at 1 : 5; 0.5% magnesium stearate was used as a lubricator. The value of FPF for SBS was 41.51؎ ؎2.22% for this formulation. Sustained release of SBS from the VPG liposomes was found in the in vitro release study. The study results offer the promising possibility of localized pulmonary liposomal SBS delivery in the anhydrous state.

Lactose characteristics and the generation of the aerosol

“…Hydration of liposome polar head groups with the hydroxyl groups of lactose leads to stabilisation, and, during dehydration, lactose protects the liposomal permeability barrier, reducing leakage of the drug from the liposomes [215].…”

Development and evaluation of a dry powder formulation of liposome-encapsulated oseltamivir phosphate for inhalation

“…The flowability of the dry powders is an important factor affecting its in vitro deposition performance (Huang et al, 2010). The value of FPF was 35.4% for this formulation, which demonstrated liposomal OP dry powders could be distributed in the lung well.…”

“…They can serve as a solubilization matrix for poorly soluble agents and act as sustained release reservoir, showing good compatibility with lung surfactant components and low local irritation to lung tissue (Drulis-Kawa & Dorotkiewicz-Jach, 2010;Chen et al, 2012). And, the development of liposomal dry powder inhalers also has been reported in the literature (Huang et al, 2010).…”

Liposome as nanocarrier: Site targeted delivery in lung cancer

“…Salbutamol sulfate (SBS) was also used as similar drug due to advanced water solubility and brisk assimilation rate. SBS was proficiently encapsulated in liposomes through vesicular phospholipid gel processes of Huang et al [92]. SBS penetration crossways to the pulmonary membrane of Asian toad was resoluted by in-vitro amendment according to Okumura et al [93].…”