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Published on: August 2, 2016
Harnessing the therapeutic potential of anticancer drugs through amorphous solid dispersions
Urvi H Gala1, Dave A Miller2, Robert O Williams3
1Molecular Pharmaceutics and Drug Delivery Division, College of Pharmacy, The University of Texas at Austin, 2409 University Avenue, Austin, TX 78712, USA; DisperSol Technologies, LLC, 111 W. Cooperative Way, Building 3, Suite 300, Georgetown, TX 78626, USA.
Abstract:
The treatment of cancer is still a major challenge. But tremendous progress in anticancer drug discovery and development has occurred in the last few decades. However, this progress has resulted in few effective oncology products due to challenges associated with anticancer drug delivery. Oral administration is the most preferred route for anticancer drug delivery, but the majority of anticancer drugs currently in product pipelines and the majority of those that have been commercially approved have inherently poor water solubility, and this cannot be mitigated without compromising their potency and stability. The poor water solubility of anticancer drugs, in conjunction with other factors, leads to suboptimal pharmacokinetic performance. Thus, these drugs have limited efficacy and safety when administered orally. The amorphous solid dispersion (ASD) is a promising formulation technology that primarily enhances the aqueous solubility of poorly water-soluble drugs. In this review, we discuss the challenges associated with the oral administration of anticancer drugs and the use of ASD technology in alleviating these challenges. We emphasize the ability of ASDs to improve not only the pharmacokinetics of poorly water-soluble anticancer drugs, but also their efficacy and safety. The goal of this paper is to rationalize the application of ASD technology in the formulation of anticancer drugs, thereby creating superior oncology products that lead to improved therapeutic outcomes.
Insights
Amorphous solid dispersions (ASDs) enhance the oral delivery of poorly soluble anticancer drugs. This formulation technology improves drug solubility, pharmacokinetics, efficacy, and safety for better cancer treatment outcomes.
Area of Science:
- Pharmaceutical Sciences
- Oncology
- Drug Delivery
Background:
- Cancer treatment faces significant challenges, particularly in effective drug delivery.
- Many anticancer drugs exhibit poor water solubility, hindering oral administration and therapeutic efficacy.
- Suboptimal pharmacokinetics and limited safety/efficacy profiles result from poor solubility of oral anticancer agents.
Purpose of the Study:
- To review challenges in oral anticancer drug delivery.
- To explore the application of amorphous solid dispersion (ASD) technology in overcoming these challenges.
- To highlight ASDs' potential to improve anticancer drug solubility, pharmacokinetics, efficacy, and safety.
Main Methods:
- Review of existing literature on anticancer drug delivery and formulation technologies.
- Analysis of amorphous solid dispersion (ASD) as a strategy for enhancing solubility of poorly water-soluble drugs.
- Discussion of the impact of ASDs on pharmacokinetic profiles, efficacy, and safety of oral anticancer agents.
Main Results:
- Amorphous solid dispersions significantly enhance the aqueous solubility of poorly water-soluble anticancer drugs.
- ASDs improve the pharmacokinetic performance of these drugs, leading to better absorption and bioavailability.
- Formulation via ASDs demonstrates potential to increase the efficacy and safety of oral anticancer therapies.
Conclusions:
- Amorphous solid dispersion technology offers a promising approach to address the limitations of oral anticancer drug delivery.
- Rational application of ASDs can lead to the development of superior oncology products with improved therapeutic outcomes.
- ASD formulation is key to unlocking the full potential of poorly soluble anticancer agents for oral administration.
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