In vitro evaluation of the effect of cyclodextrin complexation on pulmonary deposition of a peptide, cyclosporin A

International Journal of Pharmaceutics
L MatilainenPekka Jarho

Abstract

The effect of hydroxypropyl-alpha-cyclodextrin (HP-alpha-CD) complexation on in vitro pulmonary deposition of a cyclic peptide cyclosporin A (CsA) was studied. In addition, the effect of storage (32 days, 40 degrees C, 75% RH) on CsA/HP-alpha-CD complexes was studied. The complexation of CsA with CDs was evaluated by a phase-solubility method. Solid CsA/HP-alpha-CD complexes were prepared by freeze drying. Three inhalation formulations were prepared: CsA/lactose reference formulation (LF) (drug:carrier 1:364, w/w), CsA/HP-alpha-CD complex formulation (CDF) (drug:CD 1:269, w/w) and CsA/HP-alpha-CD complex/lactose formulation (CDLF) (complex:carrier 100:114, w/w). The inhalation studies were performed in vitro using Andersen Sampler (Ph. Eur.) and Taifun multi-dose dry powder inhalers (DPIs). Before the storage, the respirable fraction value (RF%) of CsA was 19.8+/-0.7%, 33.0+/-7.0% and 34.6+/-1.1% (mean+/-S.D., n=4 x 20) with LF, CDF and CDLF, respectively. When exposed to moisture (storage in a permeable polystyrene tube), the RF% values of CsA from formulations containing CsA/HP-alpha-CD complexes were lower than before the storage. However, when stored in the Taifun DPI, the RF% value of CsA from any of the formulations did n...Continue Reading

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Citations

Aug 9, 2007·Expert Opinion on Drug Delivery·Hongzhuo LiuSanming Li
Dec 30, 2009·International Journal of Pharmaceutics·Ziyaur RahmanMansoor A Khan
Apr 1, 2009·Journal of Controlled Release : Official Journal of the Controlled Release Society·L Belhadj SalemB Forbes
Jul 29, 2008·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Beatrice TrammerPetra Högger
Feb 19, 2008·International Journal of Pharmaceutics·Jie LiuZhirong Zhang
Mar 19, 2013·International Journal of Pharmaceutics·Flore DepreterKarim Amighi
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Aug 11, 2011·The Journal of Pharmacy and Pharmacology·Thorsteinn Loftsson, Marcus E Brewster
Nov 3, 2020·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·Hideyuki Sato

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