Controlled drug release system of retinoic acid

• US 6,764,698 B1
• Filed: 03/28/2001
• Issued: 07/20/2004
• Est. Priority Date: 10/01/1998
• Status: Expired due to Fees

• Current Assignee: Kwangju Institute Of Science And Technology, Shin Poong Pharmaceutical Co., Ltd.
• Original Assignee: Kwangju Institute Of Science And Technology, Shin Poong Pharmaceutical Co., Ltd.
• Inventors: Choi, Yong-Doo, Han, In-Suk, Kim, Chul-Hee, Byun, Young-Ro, Lee, Kwang-Sun, Kim, Sang-Yoon, Kim, Sun-Hee
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): Bennett, Rachel M.
• Application Number:
  US09/806,287
• Time in Patent Office: 1,210 Days
• Field of Search: 424/426, 424/489, 424/490, 424/491, 424/497, 424/501, 257/4, 257/4.1, 257/4.33, 257/4.6, 514/963, 514/725
• US Class Current: 424/489
• CPC Class Codes: A61K 9/1647 Polyesters, e.g. poly(lactide-co-glycolide)
• CPC Class Codes: A61P 35/00 Antineoplastic agents

Abstract

The present invention relates to a controlled drug release system in which a certain ratio or retinoic acid is incorporated into a microsphere comprising biodegradable polymer and amphoteric block copolymer having both hydrophilic and hydrophobic groups.

Claims

1. A controlled drug release system for retinoic acid characterized in that retinoic acid is incorporated into a microsphere prepared by mixing a biodegradable polymer, which is selected from the group consisting of poly-L-lactic acid, poly-D,L-lactic acid and poly(lactic-co-glycolic acid), and an amphiphilic AB type di-block copolymer, which is poly-L-lactic acid-polyethyleneglycol or poly(lactic acid-co-glycolic acid)-polyethyleneglycol, together, wherein the retinoic acid is selected from the group consisting of all-trans-retinoic acid, 13-cis-retinoic acid, 9-cis-retinoic acid, other retinoids and the mixture thereof, and the mixing ratio of the biodegradable polymer and the amphiphilic block copolymer is 1-20% by weight.

2. The drug release system for retinoic acid according to claim 1, wherein the mixing ratio of retinoic acid and microsphere is between 0.1˜

50 wt % based on the weight of microsphere.

3. The drug release system for retinoic acid according to claim 1, wherein the particle size of the microsphere is between 0.001 and 1000 μ

m.

4. The drug release system for retinoic acid according to claim 1, wherein the amphiphilic block copolymer comprises 1˜

20 wt % of poly-L-lactic acid-polyethyleneglycol di-block copolymer based on the total weight of the release system.

5. A pharmaceutical composition for the prevention or treatment of diseases selected from the group consisting of head and neck cancer, skin cancer, lung cancer, breast cancer, cervical cancer, bladder cancer, and acute promyelocytic leukemia comprising an effective amount of the drug release system according to claim 1, 2, 3, or 4 as an active ingredient and a pharmaceutically acceptable carrier.