Analyzing the Potential of Cyclodextrins in Advancing Drug Delivery

Highlights:

• Introduction
• Enhancing drug solubility and stability
• Improving bioavailability and targeted delivery
• Applications in oral drugs and injectable formulations

Cyclodextrins encapsulate drugs, improving their power to dissolve in blood. They make absorption of medicines better and help in precise targeting. Moreover, they minimize side effects and provide better therapeutic outcomes. As a result, cyclodextrins are paving the way for more efficient and personalized treatments, revolutionizing how we approach drug delivery in modern medicine.

Solubility and stability enhancement

Many drugs do not dissolve well in water, which limits their bioavailability. Cyclodextrin addresses this issue by forming inclusion complexes that increase the drug’s solubility. For example, β-cyclodextrin mixes ibuprofen faster, making it more effective than before. The central cavity of cyclodextrins encapsulates various hydrophobic molecules, including drugs, forming inclusion complexes. It also boosts the mixing capacity of water-soluble drugs, as the hydrophobic drug molecules are compatible with the aqueous environment. Moreover, cyclodextrin is highly valuable for improving the delivery and efficacy of pharmaceuticals. Its unique molecular structure allows it to form inclusion complexes with various drugs, enhancing their solubility and stability.

Cyclodextrins protect drugs from environmental factors such as light, oxygen, and moisture. It is particularly important for drugs that are prone to degradation. For instance, cyclodextrin complexes of the anticancer drug paclitaxel have shown improved stability compared to the free drug, extending its shelf life and effectiveness. A notable collaboration occurred in 2019 between scientists at the University of California, San Diego, and AstraZeneca, which focused on using cyclodextrins to stabilize the delivery of poorly soluble drugs, demonstrating their potential to revolutionize drug formulation and efficacy.

Improving bioavailability and targeted delivery

Bioavailability refers to the extent and rate at which the active ingredient or active moiety is absorbed and becomes available at the site of action. Cyclodextrins develops bioavailability by increasing drug solubility and protecting the drug from degradation. For instance, the use of γ-cyclodextrin has been shown to increase the bioavailability of the antihypertensive drug valsartan. A notable example of cyclodextrins in action is hydroxypropyl-β-cyclodextrin (HP-β-CD) used with the antifungal drug amphotericin B. HP-β-CD grows the dissolving capacity of amphotericin B and reduces its toxicity, making it a more effective treatment for fungal infections. This change was highlighted in a study by Santos et al. in 2023, highlighting how HP-β-CD significantly boosts drug performance and safety.

Cyclodextrins facilitate targeted drug delivery by controlling release of drugs at specific sites in the body. This is achieved through the modification of cyclodextrins to release the drug in response to environmental stimuli, such as pH changes or enzymatic activity. Cyclodextrin-based nanoparticles have been developed to deliver anticancer drugs directly to tumor cells, minimizing side effects on healthy tissues. Moreover, cyclodextrin-based drug delivery systems have been developed to target specific receptors or tissues. Research has demonstrated the successful use of cyclodextrins in targeting the delivery of gene therapies and nucleic acids, offering new possibilities for treating genetic disorders and cancers. The increasing use of drug solubility, stability, and bioavailability has significantly contributed to the expansion of the Cyclodextrins industry. According to a recently published report by Allied Market Research, it is projected to be valued at $579.6 million by 2032, growing at a CAGR of 5.7%.

Applications in oral drugs and injectable formulations

Cyclodextrins are widely used in oral drug delivery systems to enhance absorption of drugs in the gastrointestinal tract. For example, cyclodextrins in oral formulations of the antidiabetic drug glipizide have led to better therapeutic outcomes. A 2021 collaboration between researchers at the University of Michigan and Merck & Co. focused on using cyclodextrins to provide optimal effectiveness of oral medications. Additionally, a 2022 partnership between the University of Tokyo and Takeda Pharmaceuticals explored cyclodextrin-based formulations to increase the bioavailability of several drugs, demonstrating their significant impact on oral drug delivery.

In injectable formulations, cyclodextrins solubilize drugs that are less soluble in water. The antipsychotic drug risperidone improves its absorption and reduces injection-site reactions. Moreover, cyclodextrins are used in topical and transdermal drug delivery systems. They penetrate drugs through the skin and stabilizes topical formulations. In 2019, researchers at the University of Oxford and the pharmaceutical company GlaxoSmithKline collaborated to develop cyclodextrin-based solutions for better dissolving power of injectable drugs. Another significant partnership occurred in 2020 between scientists at the Massachusetts Institute of Technology and Pfizer, which focused on using cyclodextrins in injectable biological drugs.

In summary, cyclodextrins have significantly transformed the solubility, stability, and effectiveness of medicines in drug delivery. Their unique ability to form inclusions with hydrophobic drugs leads to better therapeutic outcomes, reduces side effects, and enhances patient compliance. Beyond pharmaceuticals, cyclodextrins are applied in food and cosmetics, where they help stabilize ingredients and improve product performance. Cyclodextrins is expected to develop drug-delivery technologies as R&D creates effective and innovative applications and refine formulations. 

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