Drug delivery system for the simultaneous delivery of drugs acti

Synthetic resins or natural rubbers -- part of the class 520 ser – Synthetic resins – Mixing of two or more solid polymers; mixing of solid...

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424 7817, 424 7818, 424 7831, 530811, 530812, 530815, 530816, C08G 6348, C08G 6391, A61L 901

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active

052584534

ABSTRACT:
Compositions for the treatment of cancerous tissues in warm-blooded animals containing both an anticancer drug and a photoactivatable drug attached to copolymeric carriers are made up of a member selected from the group consisting of (a) a copolymeric carrier having attached thereto both an anticancer drug and a photoactivatable drug, (b) a mixture of copolymeric carriers wherein one copolymeric carrier has attached an anticancer drug and the other copolymeric carrier has attached a photoactivatable drug and (c) a combination of (a) and (b). The anticancer drug is attached to the polymeric carrier by side-chains which are stable in the blood stream of the warm-blooded animal but susceptible to hydrolysis by lysosomal enzymes intracellularly. The photoactivatable drug is attached by either the same degradable side-chain or by a non-degradable attachment. The polymer carrier may optionally contain a targeting moiety. Upon administration polymeric macromolecules enter targeted cancer cells by pinocytosis which reduces the side effects normally elicited by the free drugs. A time lag is allowed following administration for optimal uptake of the copolymers in the cancerous tissue for the anticancer agent to begin to take effect. Then a light sources of the appropriate wavelength and energy is to activate the photoactivatable drug. The combined effect of the anticancer agent and photoactivatable drug provides greater cell destruction at reduced dosages and side effects.

REFERENCES:
patent: 5037883 (1991-08-01), Kopecek et al.
Krinick "Synthesis of N-(2-Hydroxypropyl)Methacrylamide Copolymer-Anti-Thy 1,2 Antibody-Chlorin e.sub.6 Conjugates and a Preliminary Study of Their Photodynamic Effect on Mouse Splenocytes in vitro" Makrol. Chem., 191, 839-856 (1990).
Dougherty "Photoradiation Therapy for Cutaneous and Subcutaneous Malignancies" J. of Invest., Dermatology 77: 122-124, 1981.
Kopecek et al "Targetable Photoactivatable Polymeric Drugs" J. of Cont. Release 16 (1991) 137-144.

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