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Bicalutamide Anticancer Activity Enhancement by Formulation of Soluble Inclusion Complexes with Cyclodextrins.

Author: CelestiConsuelo, CristianoMaria Chiara, De GaetanoFederica, IannazzoDaniela, IraciNunzio, PaolinoDonatella, PistaràVenerando, VenturaCinzia Anna

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Overview

This study developed inclusion complexes of bicalutamide (BCL) with hydroxypropyl-β-cyclodextrin (HP-β-CyD) and sulfobutylether-β-cyclodextrin (SBE-β-CyD) to enhance its water solubility and anticancer activity. The inclusion complexes were successfully prepared and characterized, showing improved water solubility and significantly higher antiproliferative activity against human prostate androgen-independent cell lines compared to free BCL. This suggests that HP-β-CyD and SBE-β-CyD can be used to develop liquid formulations of BCL with potential for improved oral bioavailability and even parenteral administration.
Paper Details　
Original Abstract of the Article :
Bicalutamide (BCL) is a nonsteroidal antiandrogen drug that represents an alternative to castration in the treatment of prostate cancer, due to its relatively long half-life and tolerable side effects. However, it possesses a very low water solubility that can affect its oral bioavailability. In thi...See full text at original site
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引用元：
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9687945/

データ提供：米国国立医学図書館（NLM）

Enhancing Bicalutamide's Anticancer Activity: The Power of Cyclodextrins

Bicalutamide, a nonsteroidal antiandrogen drug used to treat prostate cancer, has a significant limitation: low water solubility, which can hinder its absorption and effectiveness. This study investigates the use of cyclodextrins, a class of cyclic oligosaccharides, to improve the water solubility and anticancer activity of bicalutamide.

Cyclodextrins: A Solution for Enhanced Drug Delivery

The study successfully formed inclusion complexes of bicalutamide with hydroxypropyl-beta-cyclodextrin (HP-beta-CyD) and sulfobutylether-beta-cyclodextrin (SBE-beta-CyD). These complexes showed significantly increased water solubility compared to free bicalutamide, leading to enhanced antiproliferative activity against human prostate cancer cell lines. The research highlights the potential of cyclodextrins as a promising strategy for improving drug delivery and efficacy in cancer treatment.

Cyclodextrins: A Bridge Between Drug and Body

Imagine cyclodextrins as a caravan of camels, navigating the vast desert of the human body, carrying a precious cargo of bicalutamide. These cyclodextrins act as carriers, encapsulating the drug and facilitating its transport through the body, ensuring its safe and efficient delivery to target sites. This approach, much like a well-organized caravan, ensures that the drug reaches its destination with maximum effectiveness.

Dr.Camel's Conclusion

This study demonstrates the potential of cyclodextrin-based formulations to enhance the delivery and effectiveness of bicalutamide in prostate cancer treatment. The increased water solubility and improved anticancer activity of the inclusion complexes suggest that cyclodextrins could play a significant role in optimizing drug delivery and improving patient outcomes. The research offers a promising avenue for developing novel drug delivery systems that enhance the therapeutic efficacy of existing medications.

Date :
  1. Date Completed 2022-11-28
  2. Date Revised 2022-12-01
Further Info :

Pubmed ID

36421730

DOI: Digital Object Identifier

PMC9687945

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Languages

English

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