Polymer coating of carrier excipients modify aerosol performance of adhered drugs used in dry powder inhalation therapy

被引:20
作者
Traini, Daniela [1 ,2 ]
Scalia, Santo [4 ]
Adi, Handoko [3 ]
Marangoni, Elisabetta [4 ]
Young, Paul M. [1 ,2 ]
机构
[1] Woolcock Inst Med Res, 431 Glebe Point Rd, Glebe, NSW 2037, Australia
[2] Univ Sydney, Discipline Pharmacol, Sydney Med Sch, Sydney, NSW 2006, Australia
[3] Univ Sydney, Adv Drug Delivery Grp, Fac Pharm A15, Sydney, NSW 2006, Australia
[4] Univ Ferrara, Dept Pharmaceut Sci, I-44100 Ferrara, Italy
关键词
Dry powder inhaler (DPI); Lactose; Salbutamol sulphate; Polyvinylpyrrolidone; Ethyl cellulose; Coating; LACTOSE CARRIER; SURFACE-ENERGY; SALBUTAMOL SULFATE; ELECTROSTATIC CHARGE; ETHYL CELLULOSE; TABLET SURFACES; FILM COATINGS; PARTICLE-SIZE; ADHESION; FORMULATIONS;
D O I
10.1016/j.ijpharm.2012.08.036
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The potential of excipient coating to enhance aerosol performance of micronized drugs in carrier excipient-drug blends, used in dry powder inhalers, was investigated. Both EC (ethyl cellulose) and PVP (polyvinylpyrrolidone) were used as coating agents. Carriers were prepared via sieve fractioning followed by spray drying, with and without polymer additive. Each uncoated and coated carrier salbutamol sulphate (SS) blended systems were evaluated for particle size, morphology, drug carrier adhesion and aerosolisation performance, after blending and storage for 24 h. All carrier-based systems prepared had similar particle sizes and morphologies. The surface chemistries of the carriers were significantly different, as was drug-carrier adhesion and aerosolisation performance. Particle adhesion between SS and aerosol performance (fine particle fraction; FPF) followed the rank: PVP coated > uncoated > EC coated lactose. This rank order could be attributed to the surface energy measured by contact goniometry and related to the chemistry of lactose and each polymer. Storage did not significantly affect aerosol performance, however a rank increase in mean FPF value was observed for uncoated and EC coated lactose. Finally, the net electrostatic charge across the aerosol cloud indicated that the EC coated lactose transferred less charge to SS particles. The performance of each carrier system could be attributed to the carrier surface chemistry and, in general, by careful selection of the coating polymer, drug-carrier adhesion, electrostatic charge and aerosol performance could be controlled (C) 2012 Elsevier B.V. All rights reserved.
引用
收藏
页码:150 / 159
页数:10
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