Lipid based formulations: strategy, formulations, methods and saturation

Lipid based formulations: strategy, formulations, methods and saturation

Celkové hodnotenie

Vedecká práca
100%
Prevedenie (dizajn)
100%
Diskusná interakcia
100%
PoužívateľVedecká prácaDizajnDiskusná interakcia
MVDr. Denisa Toropilová PhD.100%100%100%
Ivana Šoltýsová100%100%100%
Mgr. Mária Suváková100%100%100%
Andrej Horňák100%100%100%
Mgr Ivana Širochmanová100%100%100%
Ing. Katarína Kaľatová100%100%100%
Mgr Barbora Selepova100%100%100%
ISBN: 978-80-972360-1-4

Lipid based formulations: strategy, formulations, methods and saturation

Ivana Šoltýsová1
1 Univerzita veterinárskeho lekárstva a Farmácie v Košiciach, Košice,
ivanasoltysova1@gmail.com

Active pharmaceutical ingredients differ by their physico-chemical properties and their bioavailability therefore varies. The most frequently used and most convenient way of administration of medicines is oral, however many drugs are little soluble in water. Thus they are not sufficiently effective and suitable for such administration. For this reason a system of Lipid Based Formulations (LBF) was developed.

Series of formulations were prepared and tested in water and biorelevant media. On the basis of selection criteria, there were selected formulations with the best emulsification potential, good dispersion in the environment and physical stability. Samples of structurally different drugs included in the Class II of the Biopharmaceutics Classification System (BCS) were obtained, namely Griseofulvin, Glibenclamide, Carbamazepine, Haloperidol, Itraconazol, Triclosan, Praziquantel and Rifaximin, for testing of maximal saturation in formulations prepared from commercially available excipients. Methods were developed for preparation of formulations, observation of emulsification and its description, determination of maximum solubility of drug samples in the respective formulation and subsequent analysis.

Saturation of formulations with drugs showed that formulations 80% XA and 20% Xh, 35% XF and 65% Xh were best able to dissolve the drugs which supports the hypothesis that it is desirable to identify limited series of formulations which could be generally applied for this purpose.

Poďakovanie: 

Astellas Pharma Europe BV, The Netherlands IAESTE Slovakaia DVM. Denisa Toropilová, PhD.; Tom de Vringer, PhD.

Zdroje: 

1. Driscoll, C.M.O., 2002: Lipid based formulations for intestinal lymphatic delivery. Eur. J. Pharm. Sci.,15, 405—415.
2. Hulling, Mu., Holm, R., Mullertz, A., 2013: Lipid-based formulations for oral administration of poorly water-soluble drugs. Int. J. Pharm., 453, 215—224.
3. Humberstone, A.J., Charman, W.N., 1995: Lipid-based vehicles for the oral delivery of poorly water soluble drugs. Adv. Drug Deliv. Rev., 25, 103—128.
4. Charman, W.N., Porter, C.J., Mithani, S., Dressman, J.B., 1997: Physicochemical and physiological mechanisms for the effects of food on drug absorption: the role of lipids and pH. J. Pharm. Sci., 86, 269—282.
5. Kalepu, S., Manthina, M., Padavala, V., 2013: Oral lipidbased drug delivery systems — an overview. Acta Pharmaceutica Sinica B, 3, 361—372. 6. Kawabata, Y., Wada, K., Nakatani, M., Yamada, S., Onoue, S., 2011: Formulation design of poorly water-soluble drugs based on biopharmaceutics classification system: Basic approaches and practical applications. Int. J. Pharm., 420, 1—10.
7. Osterberg, R.E., See, N.A., 2003: Toxicity of excipients— a food and drug administration perspective. Int. J. Toxicol., 22, 37—380.
8. Pouton, C.W., Porter, Ch.J.H., 2008: Formulation of lipid-based delivery systems for oral administration: Materials, methods and strategies. Adv. Drug Deliv. Rev., 60, 625—637.
9. Porter, C.J., Charman, W.N., 2001: In vitro assessment of oral lipid based formulations. Adv. Drug Deliv. Rev., 50, 127—147.
10. Porter, C.J., Treyaskis, N.L., Charman, W.N., 2007: Lipids and lipid-based formulations: optimizing the oral delivery of lipophilic drugs. Nature Reviews Drug Discovery, 6, 231—248.
11. Pramod, K., Peeyush, K., Rajeev, K., Nitish, K., Rakesh, K., 2010: An overview of lipid based formulation for oral drug delivery. Drug Inv. Today, 2, 390—395.
12. The United States Pharmacopoeia Convention (2009) [online]. United States Pharmacopoeia excipient verification program. 35—40. http://www.usp.org/sites/default/files/usp_pdf/ EN/products/usp2008p2supplement3.pdf
13. Walle, T., Hsieh, F., DeLegge, M.H., Oatis, J.E.Jr., Walle, U.K., 2004: High absorbtion but very low bioavailability of oral resveratrol in humans. Drug Metab. Dispos., 32, 1337—1382.
14. Wilson, C.G., Mahony, B.O., 1997: The behaviour of fats and oils in the upper G.I.Tract. Bulletin Technique Gattefosse, 90, 13−18. * S.

Diskusia

Zaujímal by ma pohľad na túto tému z hľadiska financií a ekonomiky. Aké výhody to prináša?

V tejto sfére nie som celkom doma. Avšak, tieto formy liečiv prinášajú výhodu dávkovania lieku v oveľa menšej miere, ako doposiaľ existujúce liekové formy. Predpokladajú sa teda nižšie výdavky v procese výroby, ako aj pri samotnej medikamentóznej liečbe.

Hello Ivana, I would like to ask you if the system of Lipid Based Formulations that you studied is a novel approach or had been used already. Also, have any of the modified drugs you prepared been tested for bioavailability yet? If yes, have you observed significant improvement in distribution of medications administered? Thank you for your reply :)

Thank you for the question. There are some Liquid Based Formulations which consist of Hydrophilic carrier for the drug substance (eg. Ibalgin Rapidcaps) or another forms of only one lipophilic excipient carrying a drug substance. Bioavailability of these drug substances has been studied, you can find in many databases and it is wide ranging, depending on the drug form and food administration for example. So far it was observed significant improvement just in vitro studies.