Solubilizer & Novel Excipients

Using widespread application of Drug Delivery technology, NOF supplies Solubilization Kit for hydrophobic drugs. This Kit is useful for screening of new chemical entities at initial stage.



　References

1)	Polymeric Lipid Nanosphere Constituted of Poly(2-methacryloyloxyethyl phosphorylcholine-co-n-butyl methacrylate) Kazuhiko Ishihara, Yasuhiko Iwasaki, and Nobuo Nakabayashi Polym.J. 31 1231-1236 (1999)
2)	Enhanced Solubility of Paclitaxel Using Water-soluble and Biocompatible 2-Methacryloyloxyethyl Phosphorylcholine Polymers Tomohiro Konno, Junji Watanabe, Kazuhiko Ishihara J.Biomed.Mater.Res 65A(2) 210-215 (2003)
3)	Poly(ethylene glycol) derivative of cholesterol reduces binding step of liposome uptake by murine macrophage-like cell line J-774 and human hepatoma cell line HepG2 Ishiwata H ; Sato SB ; Kobayashi S ; Oku M ; Miyajima K ; et al Chem. Pharm. Bull.; VOL 46 ISS Dec 1998, P1907-1913
4)	Niosomes containing N-(2-hydroxypropyl)methacrylamide copolymerdoxorubicin (PK1): effect of method of preparation and choice of surfactant on niosome characteristics and a preliminary study of body distribution Uchegbu IF ; Duncan R Int. J. Pharm.; VOL 155 ISS Sep 12 1997, P7-17
5)	Effect of polyoxyethyleneglycol (24) cholesterol on the solubility, toxicity and activity of amphotericin B Tasset C ; Goethals F ; Preat V ; Roland M Int. J. Pharm.; VOL 58 ISS Jan 15 1990, P41-48
6)	Distribution, metabolism and tumoricidal activity of doxorubicin administered in sorbitan monostearate (Span 60) niosomes in the mouse Uchegbu IF ; Double JA ; Turton JA ; Florence AT Pharm. Res.; VOL 12 ISS Jul 1995, P1019-1024
7)	Phase transitions in aqueous dispersions of the hexadecyl diglycerol ether (C16G2) nonionic surfactant, cholesterol and cholesteryl poly-24-oxyethylene ether: vesicles, tubules, discomes and micelles Uchegbu IF ; McCarthy D ; Schatzlein A ; Florence AT S.T.P. Pharma Sci.; VOL 6 ISS 1 1996, P33-43
8)	Effect of monomers and of micellar and vesicular forms of non-ionic surfactants (Solulan C24 and Solulan 16) on Caco-2 cell monolayers Dimitrijevic D ; Lamandin C ; Uchegbu IF ; Shaw AJ ; Florence AT J. Pharm. Pharmacol.; VOL 49 ISS Jun 1997, P611-616
9)	Polyhedral non-ionic surfactant vesicles Uchegbu IF ; Schatzlein A ; Vanlerberghe G ; Morgatini N ; Florence AT J. Pharm. Pharmacol.; VOL 49 ISS Jun 1997, P606-610
10)	A contribution to wool wax alcohol allergy. AUTH R ; PEVNY I ; GERNOT P AKTUEL DERMATOL; 10 (6). 1984 (RECD. 1985). 215-220.

　< Preparation >
The following instructions are for preparation of 5 vials of the test solution at the same time.

(1)	Weigh drugs into test tube or cuvette according to the desired concentration in the final solution. If you wish to make 1mg/mL of the final solution, weigh 12 mg of the drug, add 3mL of ethanol (select other solvent when drug is not soluble in ethanol) into the test tube, and then dissolve completely by gentle shaking.
(2)	Pipette out 500μL of the drug solution, and pour the solution into each vial of PUREBRIGHT SL Kit respectively.
(3)	Dissolve completely by shaking. Warm the vial to 50℃* to obtain a clear solution.
(4)	Evaporate the solvent from the vial according to one of the following methods a) Place the vial into vacuum chamber previously warmed to 50℃*, then evaporate the solvent under vacuum. b) Evaporate the solvent by a N2 gas stream at 50℃* over vials placed in a warm bath. Exercise caution in handling to avoid fires or accidents caused by the volatile solvent
(5)	Add 2mL of deionized water into the vial, and the dissolve completely with shaking. Add 1.8mL of deioni zed water in case of using PUREBRIGHT SL-411.

Drug in aqueous solution (e.g., 1mg/ml) is now ready.

Remarks: *Temperature may be changed depending upon the drug stability.