Use of silk protein, sericin, as a sustained-release material in the form of a gel, sponge and film.
To evaluate the usability of silk protein (sericin, SC) as a sustained-release material, the physicochemical properties of SC and the release profiles of model drugs from SC gel, sponge and film were studied. Heat aids the dissolution of SC. The molecular weight of SC tended to decrease as the heating temperature and heating time increased. The gel and sponge formed by SC were moldable and consisted of high molecular weight SC polymers (250 kDa and about 400 kDa). SC film was easily broken and exhibited elastic distortion. The addition of moisture-retaining plasticizer (glycerin and sorbitol) improved the film-forming characteristics of SC. The results suggested that SC is practical as a moldable gel and sponge, and as a tensible film. To evaluate the release profiles of small molecules, fluorescein isothiocyanate-dextran ((1) FD4, 4 kDa and (2) FD70, 70 kDa) were used as two model drugs with significantly different molecular weights, and fluorescein isothiocyanate-albumin ((3) FA, 66 kDa) was used as a charged drug. Each was formulated in SC gel, sponge and film. In each preparation, the release rate of the model drugs tended to be FA<FD70<FD4. FA, which has a large molecular weight and negative charge, was released for the longest period of time (≥1 week) from each preparation. The results suggest that SC is usable as an aqueous sustained-release material for high molecular weight drugs. Furthermore, if the drug is charged, its release can be sustained for an extended time.
Kissei Pharmaceutical Co., Ltd., Hotaka, Azumino, Japan. ayumu_nishida@pharm.kissei.co.jp
Ayumu
A
Nishida
Masaki
M
Yamada
Takanori
T
Kanazawa
Yuuki
Y
Takashima
Kiyohisa
K
Ouchi
Hiroaki
H
Okada
D000818:Animals; D012831:Bombyx / Q000737:chemistry*; D003692:Delayed-Action Preparations / Q000737:chemistry*; D005782:Gels / Q000737:chemistry*; D004364:Pharmaceutical Preparations / Q000008:administration & dosage*; D047030:Sericins / Q000737:chemistry*
D003692:Delayed-Action Preparations; D005782:Gels; D004364:Pharmaceutical Preparations; D047030:Sericins