Pharmaceutical Formulation for Poorly Water Soluble Camptothecin Analogues
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Nanosized Technological Approaches for the Delivery of Poorly Water Soluble Drugs
A major hurdle in pharmaceutical formulation is water insolubility of most of drugs affecting their stability and bioavailability. If the drug is also insoluble in organic medium, it is difficult to deliver it in a sufficiently bioavailable form and hence it is a great challenge to formulation researchers to overcome such difficulty. Although some approaches are available for enhancing th...
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Camptothecin is a natural, water-insoluble alkaloid produced by two Asian trees, Camptotheca acuminata and Mappia foetida. In the 1970s, preliminary clinical trials with camptothecin demonstrated promising antitumor activity, for example, in gastric cancer. Unfortunately, there were also severe side effects, including poorly predictable hemorrhagic cystitis, gastrointestinal toxicities and myel...
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Water-soluble 20(S)-glycinate esters of two highly potent 10,11-methylenedioxy analogues of camptothecin (CPT) have been synthesized and evaluated for their ability to eradicate human breast cancer tumor xenografts. The glycinate ester moiety increases the water solubility of the 10,11-methylenedioxy analogues 4-16-fold. However, in contrast to CPT-11, a water-soluble CPT analogue that was rece...
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Low solubility compounds show dissolution rate limited absorption and hence poor absorption, distribution and target organ delivery. Improvement of aqueous solubility in such a case is valuable goal to improve therapeutic efficacy. Complexation with CDs by different methods like physical mixing, melting, kneding, spray drying, freeze drying, co-evaporation has been reported to enhance the solub...
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تاریخ انتشار 2017