Preparation of drug-loaded small unilamellar liposomes and evaluation of their potential for the treatment of chronic respiratory diseases

Publication date: 10 July 2018 Source:International Journal of Pharmaceutics, Volume 545, Issues 1–2 Author(s): Vincenzo De Leo, Silvia Ruscigno, Adriana Trapani, Sante Di Gioia, Francesco Milano, Delia Mandracchia, Roberto Comparelli, Stefano Castellani, Angela Agostiano, Giuseppe Trapani, Lucia Catucci, Massimo Conese The aim of the present investigation was to evaluate the influence of liposome formulation on the ability of vesicles to penetrate a pathological mucus model obtained from COPD affected patients in order to assess the potential of such vesicles for the treatment of chronic respiratory diseases by inhalation. Therefore, Small Unilamellar Liposomes (PLAIN-LIPOSOMEs), Pluronic® F127-surface modified liposomes (PF-LIPOSOMEs) and PEG 2000PE-surface modified liposomes (PEG-LIPOSOMEs) were prepared using the micelle-to-vesicle transition (MVT) method and beclomethasone dipropionate (BDP) as model drug. The obtained liposomes showed diameters in the range of 40–65 nm, PDI values between 0.25 and 0.30 and surface electric charge essentially close to zero. The encapsulation efficiency was found to be dependent on the BDP/lipid ratio used and, furthermore, BDP-loaded liposomes were stable in size both at 37 °C and at 4 °C. All liposomes were not cytotoxic on H441 cell line as assessed by the MTT assay. The liposome uptake was evaluated through a cytofluorimetric assay that showed a non-significant reduction in the internalization of PEG-LIPOSOM...
Source: International Journal of Pharmaceutics - Category: Drugs & Pharmacology Source Type: research