Journal
INTERNATIONAL JOURNAL OF PHARMACEUTICS
Volume 498, Issue 1-2, Pages 234-244Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2015.12.029
Keywords
High speed electrospinning; Amorphous solid dispersion; Long-term stability; Raman mapping; Oral drug delivery
Categories
Funding
- New Szechenyi Development Plan [TAMOP-4.2.1/B-09/1/KMR-2010-0002]
- OTKA research fund [K112644, PD108975]
- MedInProt Synergy Program
- Janos Bolyai Research Scholarship of the Hungarian Academy of Sciences
Ask authors/readers for more resources
In this research the long-term stability (one year) of amorphous solid dispersions (ASDs) prepared by high speed electrospinning was investigated at 25 degrees C/60% relative humidity (RH) (closed conditions) and 40 degrees C/75% RH (open conditions). Single needle electrospinning and film casting were applied as reference technologies. Itraconazole (ITR) was used as the model API in 40% concentration and the ASDs consisted of either one of the following polymers as a comparison: polyvinylpyrrolidone-vinyl acetate 6: 4 copolymer (no hydrogen bonds between API and polymer) and hydroxypropyl methylcellulose (possible hydrogen bonds between oxo or tertiary nitrogen function of API and hydroxyl moiety of polymer). DSC, XRPD and dissolution characteristics of samples at 0, 3 and 12 months were investigated. In addition, Raman maps of certain electrospun ASDs were assessed to investigate crystallinity. A new chemometric method, based on Multivariate Curve Resolution-Alternating Least Squares algorithm, was developed to calculate the spectrum of amorphous ITR in the matrices and to determine the crystalline/amorphous ratio of aged samples. As it was expected ITR in single needle electrospun SDs was totally amorphous at the beginning, in addition hydroxypropyl methylcellulose could keep ITR in this form at 40 degrees C/75% RH up to one year due to the hydrogen bonds and high glass transition temperature of the SD. In polyvinylpyrrolidone-vinyl acetate matrix ITR remained amorphous at 25 degrees C/60% RH throughout one year. Materials prepared by scaled-up, high throughput version of electrospinning, which is compatible with pharmaceutical industry, also gained the same quality. Therefore these ASDs are industrially applicable and with an appropriate downstream process it would be possible to bring them to the market. (C) 2015 Elsevier B.V. All rights reserved.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available