Cyclodextrins (CD) can be easily modified to obtain CD derivatives. Modified cyclodextrins demonstrate better physicochemical properties and encapsulation capabilities than virgin cyclodextrins, which makes them more appropriate for their planned applications. The market features over 11,000 different cyclodextrin derivatives, and Alfa Chemistry provides industrial-scale availability of diverse cyclodextrin variants. Our specialized synthesis laboratory enables us to deliver any specific cyclodextrin derivatives that our customers need besides our standard offerings.
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Cyclodextrin derivatives are functional compounds obtained by chemically modifying the hydroxyl group or other active sites of natural cyclodextrins (α-CD, β-CD, γ-CD, etc.). Natural cyclodextrins are cyclic oligosaccharides consisting of 6-12 D-glucose units linked by α-1,4-glycosidic bonds and have a unique “truncated cone” structure: the inner cavity is hydrophobic and the outer surface is hydrophilic.
Key Properties:
Amphiphilic
Hydroxyl groups on the outer surface make it hydrophilic, and C-H bonds and glycosidic oxygen atoms in the inner cavity form hydrophobic regions.
Size Selectivity
The inner cavity diameters of α-CD, β-CD, and γ-CD are 0.5-0.8 nm, 0.6-0.9 nm, and 0.7-1.0 nm, respectively, which are suitable for encapsulating molecules of different sizes.
Chemical Modifiability
The hydroxyl groups (C-2, C-3, C-6 positions) of cyclodextrins can be introduced into alkyl, sulfonic acid, hydroxypropyl, and other groups by substitution reaction, which can significantly change their solubility and function.
Natural cyclodextrin has a unique "truncated cone" structure: the inner cavity is hydrophobic and the outer surface is hydrophilic. This structure enables it to form inclusion complexes with various molecules through non-covalent interactions (such as hydrophobic interaction, hydrogen bonding, van der Waals forces, etc.), thereby improving the solubility, stability or bioavailability of the guest.
It consists of 6 glucose units with a diameter of about 5.0 nm and a lumen diameter of 0.7 nm, and is highly hydrophobic and suitable for encapsulating smaller molecules.
It is composed of 7 glucose units with a diameter of about 5.8 nm and a lumen diameter of 0.7 nm. It is the most widely used type of cyclodextrin with a good balance of water solubility and hydrophobicity.
It is composed of 8 glucose units with a diameter of about 6.4 nm and a lumen diameter of 0.7 nm; it is slightly larger than β-CD and is suitable for encapsulating larger molecules.
Hydroxypropyl cyclodextrins include 2-hydroxypropyl-α-cyclodextrin, 2-hydroxypropyl-β-cyclodextrin, and 2-hydroxypropyl-γ-cyclodextrin, which are hydroxyalkylated derivatives of natural cyclodextrins. The introduction of hydroxypropyl groups resulted in a significant increase in water solubility and selectivity for guest molecules. With extremely high water solubility (>500 g/L, 20 °C) and low hemolysis, hydroxypropyl-β-CD (HP-β-CD) has been approved by the FDA for use in injectable formulations, making it the most promising pharmaceutical cyclodextrin material available today.
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Sulfobutyl ether cyclodextrins are anionic sulfonic acid substituted cyclodextrins, of which the common substitution degree of sulfobutyl ether-β-cyclodextrin (SBE-β-CD) is 4 and 7. Compared with β-CD, its solubility, encapsulation ability, and safety have been improved, and it is widely used to improve the solubility and stability of the drug, to reduce irritation, to mask the bad smell, and to apply in targeting formulations.
View ProductsMethyl cyclodextrins are modified by alkylation to improve the stereoselectivity of the molecule. β-Cyclodextrins can be substituted with methyl groups at the C2, C3, and C6 positions, and the degree of substitution affects their water-solubility, fat-solubility, and encapsulation ability. Randomly methylated β-CDs exhibit better water solubility, encapsulation ability, and acid stability than natural β-CDs, making them more widely used in drug delivery.
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Hydroxypropyl Cyclodextrin (HP-CD)
Sulfobutyl Ether Cyclodextrin (SBE-CD)
Methyl Cyclodextrin (M-CD)
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Enhance Solubility & Stability with Cyclodextrin Derivatives!
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Request a QuoteChemical modifications to cyclodextrin derivatives produce enhanced water solubility and stability while adapting their cavity dimensions, which makes them ideal for areas such as drug delivery.
Enhanced Water Solubility
The natural β-CD exhibits restricted water solubility because of its hydroxyl group distribution, but its derivatives, such as HP-β-CD and SBE-β-CD, show greatly improved solubility for high-solubility demanding formulations like injectables. In addition, methylated derivatives are both hydrophilic and hydrophobic, which not only enhance drug solubility, but also promote transmembrane absorption and improve bioavailability.
Optimization of Cavity Adaptation
Modifying cyclodextrins with different substituents allows for adjustments in their hydrophobicity and cavity size to fit various drugs. α-CD is suitable for aliphatic hydrocarbons, β-CD has a higher affinity for aromatic compounds, and γ-CD can encapsulate larger molecules (e.g.e.g. steroids). Further modifications (e.g., carboxymethyl-β-CD) can improve the binding ability to charged molecules, expanding to macromolecular delivery such as proteins and nucleic acids.
Stability Enhancement
Through encapsulation, cyclodextrin derivatives protect drugs against photo-, thermal-, and oxidative degradation, which enhances drug stability. Cosmetic shelf life can be significantly extended through the use of CD inclusion complexes with vitamin drugs. CD derivatives in drug delivery systems minimize gastric acid degradation while increasing the oral formulation's bioavailability, which results in better therapeutic outcomes.
To meet customers' diverse needs for cyclodextrin derivatives, we provide comprehensive services, including analytical services and custom synthesis.
CD analysis is essential. And the complexity of CD derivatization requires more comprehensive analytical methods. With our comprehensive CD analysis services, customers are able to make sure products meet their requirements.
We have the ability to provide a full range of customized synthesis services for CDs, designing different synthesis routes according to the specific needs of customers, and providing CD derivatives with desired structures.
The following case studies demonstrate how our products have led to significant technological breakthroughs and economic benefits in real-world applications.
Customer background: A pharmaceutical company develops oral antiviral drug formulations while working to enhance the solubility and bioavailability of drugs with hydrophobic properties.
Product: Sulfobutylether-Beta-Cyclodextrin Sodium Salt (Catalog CD182410000)
Application: During antiviral drug development, researchers observed that water solubility of the active ingredient was insufficient which impacted the drug's effectiveness. This negatively charged cyclodextrin derivative can create an inclusion complex with hydrophobic drugs to both enhance their water solubility and stability while preventing toxic side effects associated with traditional solubility enhancers. The study demonstrated that the use of SBE-β-CD significantly improved drug solubility and exhibited enhanced release properties during the in vitro dissolution testing.
Background: A biotechnology firm focuses its research efforts on studying the stability of recombinant proteins together with antibody drugs.
Product: Methyl-Beta-Cyclodextrin (Catalog CD128446366)
Application: During the storage stability assessment of an antibody drug, customers identified that low-temperature freeze-drying conditions caused aggregation and denaturation, which impacted the drug's activity. SBE-Beta-CD, as a negatively charged cyclodextrin derivative, can form an inclusion complex with the hydrophobic drug to improve its solubility and stability in water, and at the same time, avoiding the toxic side effects that may be caused by traditional solubilizers. Experimental data confirms that when methyl-β-CD is incorporated into the antibody formulation, it remains highly active and stable throughout lyophilization and re-solubilization for successful long-term storage and transport.
Customer background: An ophthalmic pharmaceutical company focuses on the research and development of ocular drug delivery systems, seeking to improve the solubility and transdermal absorption of active ingredients.
Product Sourced: (2-Hydroxypropyl)-Beta-Cyclodextrin (Catalog CD128446355)
Research Application: The pharmaceutical company creates an ophthalmic solution to treat glaucoma using an active pharmaceutical ingredient (API) that is a small hydrophobic molecule whose low solubility hinders its ocular bioavailability. HP-β-CD inclusion complex formation resulted in improved aqueous solubility for the API and demonstrated higher transcorneal absorption in cellular experiments. The compound HP-β-CD demonstrated excellent biocompatibility with ocular tissues and caused no irritation, which helped increase the formulation’s safety and effectiveness.
*All products are intended for scientific use only and are not intended for human therapeutic, diagnostic, or other pharmaceutical use. You can reach out to us for additional product information or technical support.
Are your cyclodextrin derivatives available for drug delivery?
Yes, our cyclodextrin derivatives are widely used in drug delivery systems to improve drug solubility and bioavailability. In particular, methylated, hydroxypropylated, and sulfobutylated cyclodextrins excel at improving drug solubility.
Are cyclodextrin derivatives suitable for food and cosmetics?
Of course! β-Cyclodextrin and its derivatives are used in a wide range of food and cosmetic applications, e.g., for encapsulating flavors, stabilizing active ingredients, or improving the solubility of formulations. The food- and cosmetic-grade cyclodextrins we offer meet the relevant safety standards.
How soluble are your cyclodextrin derivatives?
It depends on the specific type. For example, hydroxypropyl-β-cyclodextrin (HP-β-CD) and sulfobutyl-β-cyclodextrin (SBE-β-CD) have good water solubility for water-soluble drugs and biopharmaceutical applications, whereas pristine β-cyclodextrins have lower water solubility.
Do you offer GMP-compliant cyclodextrin derivatives?
Yes, we offer specific GMP-compliant cyclodextrin derivatives suitable for the stringent quality requirements of the pharmaceutical industry. For specific needs, please feel free to contact our technical team.
How do I select the right cyclodextrin derivative for my research or product?
Choosing the right cyclodextrin derivative depends mainly on the physicochemical properties of the target compound, solubility requirements, and the final application. We provide technical support to help you find the most suitable product.
Do you offer bulk supply?
Yes, we support small-scale research-grade to industrial-scale bulk supply to ensure consistent quality and a reliable supply chain. Feel free to inquire about specific needs; we can provide customized services.
What are the storage conditions for cyclodextrin derivatives?
Most cyclodextrin derivatives should be stored in a cool, dry environment, avoiding heat and humidity. Certain highly hydrophilic derivatives are more sensitive to humidity and are recommended to be stored in sealed containers to maintain their optimal performance.
*You can get professional answers by reaching out to our technical team if you have additional questions.
Alfa Chemistry is the global leading manufacturer of cyclodextrins. We are ready to supply cyclodextrin series products for customers, from small batch to large batch orders. Your success is our greatest priority and your needs are unique. We would love to better understand your needs and connect you with our experts.
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