Planta Med 2014; 80 - P2N2
DOI: 10.1055/s-0034-1394822

Spray freeze dried lipid nanostructures containing Copaifera langsdorfii Desf. extracts

A Costa-Machado 1, A Lanchote 1, L Freitas 1
  • 1Faculdade de Ciências Farmacêuticas de Ribeirão Preto – USP, NPPNS

Copaifera langsdorffii Desf, also known as copaiba is a Brazilian native tree which antitumor activity was recently reported for its leaves extracts. To give better selectivity to this plant extract the development of new structures such as liposome must be explored. Techniques such as freeze drying are usually applied to increase LNS stability [1], but process studies regarding LNS spray freeze drying (SFD) are rarely found [2]. This work aimed to study and compare the properties of LNS before and after SFD. The LNS were obtained by the sonication of lipid film. Mannitol was used as cryoprotector. The SFD parameters evaluated were: the lipids' concentration (C) and the molar ratio of lipids to mannitol (Lip:Man). A 22 full factorial design with a central point was used. The responses evaluated were size (DP), polidispersivity index (PDI), zeta potential (ZP) and the drying yield (θ). The ANOVA analysis did not present significant effects (α= 0.05%) indicating that C and Lip:Man or their interaction did not affect the DP, PDI, ZP and θ. The DP remained around 200nm before and after SFD. The SFD showed to be a good technique to dry LNS keeping their properties and probably being a good alternative to avoid the leakage of the drug and physico-chemical instability. The factorial design was an adequate tool to study this process.

Acknowledgements: FAPESP (2011/20872 – 7 and 2013/16268 – 2), CAPES and CNPq.

Keywords: antitumoral, liposomes, spray freeze drying, size, polidispersivity, stability

References:

[1] vanWinden ECA, Crommelin DJA. Long term stability of freeze-dried, lyoprotected doxorubicin liposomes. Eur J Pharm Biopharm 1997; 43: 295 – 307.

[2] Cheow WS, Ng MLL, Kho K, Hadinoto K. Spray-freeze-drying production of thermally sensitive polymeric nanoparticle aggregates for inhaled drug delivery: effect of freeze-drying adjuvants. International Journal of Pharmaceutics 2011; 404: 289 – 300.

[3] Rowe RC, Sheskey PJ, Owen SC. Handbook of pharmaceutical excipients. 5th ed. London/Chicago: Pharmaceutical Press and American Pharmacists Association; 2006.