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Pharmaceutical Cyclodextrin Development

Overview

Cyclodextrins play an important role in the pharmaceutical industry due to their amphiphilic properties and excellent biocompatibility. CD BioGlyco looks forward to providing our customers with professional and rapid solutions in the field of pharmaceutical cyclodextrin development.

The Importance of Cyclodextrins in Pharmaceutical Technology

The central cavity of the cyclodextrin molecule offers a somewhat lipophilic nanoenvironment in which appropriately sized drug parts (or even small drug molecules) can be entered and contained. Therefore, cyclodextrins have been of particular importance in drug delivery and pharmaceutical technologies. For example, the synthesis of novel surface active cyclodextrin derivatives is applied to drug delivery systems. Certainly, cyclodextrins enhance the apparent solubility of drugs as the result of the formation of cyclodextrin/drug inclusion complexes. However, the complexation can also protect drugs from heat, light, hydrolysis, and oxidation, thereby improving the stability of formulations. In other cases, many active pharmaceutical ingredients have undesirable taste and odor, which can lead to low patient compliance, thereby compromising the treatment efficiency, especially for geriatric and pediatric populations. It allows the manipulation of volatile compounds, reduces unpleasant tastes and odors, and decreases the effect of irritating compounds. Moreover, cyclodextrins can modify the release rate of drugs working as excipients for immediate or sustained release. In addition, cyclodextrins are used for optimizing the bioavailability of drugs through chemically modified cyclodextrin derivatives, and the combination of different types of building blocks. However, in recent years cyclodextrins have been shown to participate in various types of non-inclusion complexes with, for example, organic salts and water-soluble polymers. They have also been shown to form aggregates, either alone or in combinations with other excipients. These aggregates can form dispersed drug delivery systems such as micro-and nanoparticles.

Key Technologies

Cavity engineering; AI-driven binding prediction; Precision analytics (XRD/ITC/HPLC-ELSD); Stimuli-responsive carriers (pH/redox-triggered)

Three Acknowledged Applications of Pharmaceutical Cyclodextrins

Three Acknowledged Applications of Pharmaceutical Cyclodextrins

Our Services

  • The preparation of sulfonated cyclodextrins. Sulfonated cyclodextrins can reduce the infectivity of HIV and stop viral replication in vitro.
  • The synthesis/production of cyclodextrins and their derivatives. Cyclodextrins can be prepared as aqueous for practically any route of administration, such as oral administration, parenteral administration, and ocular administration.
  • Cyclodextrin-based polymeric materials, such as hydrogels and nanoparticles.
  • Cyclodextrins can be used as complexing agents to enhance the solubility, stability, and bioavailability of a variety of drugs.
  • Cyclodextrins binding cholesterol may reduce viral infectivity.

Publication Data

DOI.: 10.5772/intechopen.108078

Journal: Cyclodextrins-Core Concepts and New Frontiers

Published: 2022

Results: The authors provide a comprehensive overview of cyclodextrins, covering their fundamental chemistry, structure (α-, β-, γ-cyclodextrinss), properties, and mechanisms of host-guest inclusion complexation, with specific emphasis on molecular dynamics driving the complex formation. They detail how cyclodextrin derivatization (e.g., HP-β-cyclodextrin, SBE-β-cyclodextrin) improves solubility and functionality. The chapter extensively reviews the applications of cyclodextrins and their complexes in enhancing key drug properties: solubility, dissolution, stability (photo/thermal), permeability, safety (reduced irritation/toxicity), and controlled release profiles. Furthermore, the authors discuss the utilization of cyclodextrins across various drug delivery routes, including oral, ocular, nasal, and transdermal systems. A significant focus is placed on novel cyclodextrin-based drug delivery approaches, particularly highlighting the development and advantages of lipid-based nanosystems (e.g., micelles, nanosponges, nanoparticles, nanovesicles) for targeted and efficient delivery in treating diseases like cancer, diabetes, and hypertension. The authors conclude that cyclodextrins, due to their unique structure and ability to form inclusion complexes, serve as versatile pharmaceutical excipients capable of significantly improving drug performance and enabling advanced delivery strategies.

Workflow

Our development process integrates advanced analytics and tailored formulations:

Candidate Screening & Feasibility

Our screening process begins with computational modeling, such as molecular docking, to predict drug-cyclodextrin inclusion complex formation, particularly for poorly soluble drugs. This is complemented by high-throughput solubility/stability assays to evaluate solubility enhancement and pH/thermal stability under varied conditions.

Cyclodextrin Selection & Optimization

We select natural cyclodextrins or modified derivatives based on safety profiles and solubility requirements. Optimization involves structure-activity relationship (SAR) studies to refine substituents, enhancing properties like renal clearance or tumor-specific targeting.

Formulation Development

Complexation techniques—including kneading, co-precipitation, and freeze-drying—are employed to form stable drug-cyclodextrin inclusion complexes. These complexes are then integrated into tailored dosage forms such as oral tablets, injectables, nasal sprays, or ocular drops using cyclodextrin carriers.

In Vitro/In Vivo Validation

Validation includes in vitro release kinetics profiling and in vivo animal studies to assess biodistribution and safety parameters.

Our workflow. (CD BioGlyco)

Advantages

  • We synthesize novel cyclodextrin derivatives to optimize drug binding kinetics and release profiles.
  • High complexation efficiency is ensured through real-time quality control via HPLC-ELSD and XRD monitoring throughout the manufacturing process.
  • Our development process transitions compounds from mg-scale R&D — involving molecular modeling and phase solubility studies — to kg-scale production.

Associated Services

Frequently Asked Questions

CD BioGlyco offers integrated solutions from the design, synthesis, and modification of pharmaceutical cyclodextrins to applications. If you are interested in our services, please contact us for more information.

Reference

  1. Yousaf, R.; et al. Cyclodextrins: an overview of fundamentals, types, and applications. Cyclodextrins-Core Concepts and New Frontiers. (Open Access)
This service is for Research Use Only, not intended for any clinical use.
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CD BioGlyco is a world-class biotechnology company with offices in many countries. Our products and services provide a viable option to what is otherwise available.

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