title: Release stability of 5-fluorouracil liposomal concentrates, gels and lyophilized powder.
abstract: Possible leakage of 5-fluorouracil from stable plurilamellar vesicles was monitored during storage of the liposomal concentrates, gels and lyophilized powders. Changes in release profile of dibucaine were taken as indicator of instability. Release profiles were obtained using the dialysis technique for a freshly prepared liposomal concentrate, gel or reconstituted lyophilized powder (zero time) and storage for one, two and four weeks in well closed tubes at 4 degrees C for the liposomal concentrate or gel and at 25 degrees C for liposomal lyophilized powder. Aiming at increasing stability of 5-fluorouracil liposomal dispersion, freshly prepared liposomal concentrates were directly incorporated in hydroxypropyl methylcellulose gel. Stability release profiles of liposomal gels and concentrates indicated a significant increase in stability of liposomal formulations. Also, lyophilization increases the shelf life of liposomes by preserving it in a dry form as a lyophilized cake to be reconstituted immediately prior to administration or direct incorporation into a final dosage form. Release and physico-chemical stability studies showed superior potentials of the lyophilized product after reconstitution in comparison to concentrate and gel forms. It could be concluded that lyophilization of liposomes loaded with a water-soluble drug such as 5-fluorouracil could significantly increase the stability of the liposomal vesicles and decrease leakage from it.
authors.affiliation: Liposome Research Laboratory (LRL), Department of Pharmaceutics, Faculty of Pharmacy, University of Alexandria, Egypt. nounousomes@gmail.com
authors.forename: Mohamed Mahmoud
authors.initials: MM
authors.lastname: Nounou
authors.forename: Labiba Khalil
authors.initials: LK
authors.lastname: El-Khordagui
authors.forename: Nawal
authors.initials: N
authors.lastname: Khalafallah
mesh_terms: D000964:Antimetabolites, Antineoplastic / Q000008:administration & dosage* / Q000737:chemistry; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D016503:Drug Delivery Systems; D005472:Fluorouracil / Q000008:administration & dosage* / Q000737:chemistry; D005612:Freeze Drying; D005782:Gels; D011208:Powders; D013056:Spectrophotometry, Ultraviolet
chemical_list: D000964:Antimetabolites, Antineoplastic; D005782:Gels; D011208:Powders; D005472:Fluorouracil