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 A New Class of CD Polymers

Our CD based small drug carrier has consistently out-performed hydroxypropyl cyclodextrin (HPCD), an FDA approved excipient (solubilizer) for injection (Sporanox® Injection, Janssen Pharmaceutical).  Our CD carrier is also comparable as an excipient to Captisol®, the leading product from Cydex, Inc., Overland Park, KS.  Captisol® is a mixture of derivatized CD monomers now used as an excipient by several pharmaceutical companies for a variety of drugs (see website; cydexinc.com).

Our higher molecular weight CD carrier is virtually nontoxic and complexes with several anticancer drugs with higher affinity than Captisol® on a molar basis.

The technology platform for small drug carriers is made from cyclodextrin (CD) derivatives. 

 

Summary of CD Carrier Properties.

 

The average mw ranges available between 4000 and 10,000 kDa.

 

The carrier has been shown to complex with and/or solubilize several drugs.

Camptothecin; Cyclosporin A (CsA); DHEA; Mitoxantrone (MTN); Prednisolone; Taxol

 

The stability of the drug-loaded carrier determined by dialysis.

MTN-carrier:               less than 2% loss after 24 hours in human plasma followed by 50% EtOH dialysis.

CsA-carrier:                 26% loss after 24 hours in human plasma followed by 50% EtOH dialysis.

 

Cell uptake in vitro.

MTN-carrier:               30-40% higher than free drug after 8 hours.

 

No toxicity in vitro. Toxicity in vivo (rats injected I.P.) with MTN-carrier:

None, based on organ weights and total weight gain comparable to controls.

 

Organ uptake in vivo (heart, kidney, liver, spleen; rats injected I.P.).

Initial experiment showed lower uptake of MTN-carrier compared to free drug.

 

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