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Journal of Bioactive and Compatible Polymers
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Macrophage Activation by Poly(maleic acid-alt-2-cyclohexyl-1,3-dioxap-5-ene) Encapsulated in Polysaccharide-Coated Liposomes

Toshinori Sato

Laboratory of Artificial Cell Technology Department of Industrial Chemistry Faculty of Engineering, Nagasaki University Nagasaki 852, Japan

Kazuyuki Kojima

Laboratory of Artificial Cell Technology Department of Industrial Chemistry Faculty of Engineering, Nagasaki University Nagasaki 852, Japan

Taka-Aki Ihda

Laboratory of Artificial Cell Technology Department of Industrial Chemistry Faculty of Engineering, Nagasaki University Nagasaki 852, Japan

Junzo Sunamoto

Laboratory of Artificial Cell Technology Department of Industrial Chemistry Faculty of Engineering, Nagasaki University Nagasaki 852, Japan

Raphael M. Ottenbrite

Department of Chemistry Virginia Commonwealth University Richmond, VA 23284, U.S.A.

An increase in the efficiency of macrophage activation has been tried by en capsulating potent polyanionic polymer immunomodulators into polysac charide-coated liposomes. For this purpose, several alternating copolymers of maleic acid (MA) and itaconic acid (IT) with 2-cyclohexyl-1,3-dioxap-5-ene (CDA), styrene (ST), and other monomers have been synthesized and frac tionated.

First, the interaction between the liposomes and polyanionic polymers was investigated. As a result, poly(maleic acid-alt-2-cyclohexyl-1,3-dioxap-5-ene) (MA-CDA) was found to be the best candidate for encapsulating in the liposome while poly(itaconic acid-alt-styrene)(IA-ST) strongly perturbed these vesicles.

Based on these results, MA-CDA was encapsulated in the mannan derivative- coated liposomes and the macrophage activation activity was evaluated from the superoxide production of the activated macrophages in vivo. Compared with the administration of free MA-CDA, the maximum in the superoxide pro duction appeared faster (2 h after injection) and the activity was significantly increased.

Journal of Bioactive and Compatible Polymers, Vol. 1, No. 4, 448-460 (1986)
DOI: 10.1177/088391158600100403
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Y. Ohya, J.-I. Murata, T. Nishimoto, and T. Ouchi
Synthesis of a MDP Analogue/Chitin Conjugate That Stimulates Cultured Macrophages
Journal of Bioactive and Compatible Polymers, January 1, 1993; 8(4): 351 - 364.
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