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

Abstract

(2015) Development and evaluation of a dry powder formulation of liposomeencapsulated oseltamivir phosphate for inhalation, Drug Delivery, 22:5, 608-618, DOI: 10.3109/10717544.2013 AbstractThis study aims to develop oseltamivir phosphate (OP) liposomes as inhalation powders by spray-drying based on the single factor investigation, which was mainly composed of lactose, L-leucine and mannitol. It was found that the ratio of OP and liposomes (1:10), inlet temperature (110 C) and airflow rate (2.3 mL/min) showed optimized physical properties of OP liposomes. Deposition was evaluated after the aerosolization of powders at 600 L/h via the Aerolizer Õ into a twin-stage impinger. The concentrations of OP and oseltamivir carboxylate (OSCA) in rats plasma using LC-MS have been determined and performed via pharmacokinetic software DAS 2.0 package. The liposomal OP dry powders displayed an average particle size around 3.5 mm with fine particle fraction (FPF ¼ 35.40%). In vitro evaluation demonstrated a sustained release pattern accounting for 20% drug release compared to that of OP solution up to 90% drug release in 2 h. And the cumulative release percentage was up to 50% in 20 h. Atrioventricular fitting results indicated that all preparations were best fitted with a two-compartment model. There was a significant difference in MRT, C max and T max (p50.01) between the two groups of liposomal OP dry powders and OP solution with t-test, which indicated that the drug released slowly from liposomal OP dry powders in the lung. To sum up, dry powders formulation of liposome-encapsulated OP for inhalation was suitable for pulmonary administration, which offering the opportunity to reduce dosing frequency.

Nano-based anti-tubercular drug delivery: an emerging paradigm for improved therapeutic intervention

“…LPs are known to be engulfed by the macrophagic cells to meet their fate, hence being a probable candidate for anti-TB drugs since Mtb invests the macrophages. These attributes account for their versatile nature and urge for further exploration [66,67]. Liu et al designed thermoresponsive LP in the hydrogel system for delivering INH at the target site for bone TB.…”

A Liposomal Formulation for Improving Solubility and Oral Bioavailability of Nifedipine

“…Spray-drying was used to prepare proliposomes because nifedipine was not very sensitive to brief exposure to high temperature [15]. We were concerned that the high temperature in the process of spray-drying might destroy the liposomal membrane, so we investigated the addition of carriers (mannitol, sorbitol, and lactose) and selected mannitol as a carrier to protect liposomes from agglomerating in the process of spray drying [15,16].…”

Synthetic Advancement of Neuraminidase Inhibitor “Tamiflu”

“…Tamiflu doses are prepared in the dry powder form for inhalation with sustain release and instant release form ( up to 100 % within 60 min) by compression coating technique as well as pediatric friendly doses …”