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Hydroxypropyl-beta-cyclodextrin inclusion technology principle and release objects

2020-01-18 17:09:24 Xinda Biotechinology Read

Hydroxypropyl-beta-cyclodextrin inclusion technology principle and release objects

Inclusion Technique refers to a molecule to be entrapped within the pore structure of another molecule to form a clathrate (inClusion Compound) technology. This is the main clathrate molecules (host mo1eCule) and a guest molecule (guest moleCule) adduct composed of two components, the main structure of the molecule has a larger hole, sufficient to accommodate the guest molecule, including, forming molecular capsule ( mo1eCule Capsule).

Cyclodextrin and its derivatives in general and non-covalent binding cavity formed by the clathrate the guest molecule. Inclusion reaction is a dynamic process, constantly guest molecules with a cyclodextrin compound, but also continue to complex solutions. Control of the reaction temperature, substrate concentration, pH and other reaction conditions, the reaction to the direction of transfer in favor of complex, will get more clathrate. Hydroxypropyl cyclodextrin cyclodextrin more than the original with a suitable guest molecules form inclusion complexes as hydroxypropyl substituted 2,3-hydroxyl H atoms after increasing the length of the cyclodextrin cavity, hydroxypropyl on hydroxy may also be the guest molecules form new hydrogen bonds, increasing the stability of inclusion. Most studies show that the main hydroxypropyl cyclodextrin and guest molecules form 1: 1 inclusion complex, but also the formation of 2: 1 clathrate, or to form oligomers reported.

Part of the purpose and object of cyclodextrins form inclusion complexes is to protect, sustained or solubilization, in this case, the guest molecules eventually released from the cyclodextrin. Studies have shown that the main factors that cause or accelerate the release of the guest molecules and competitive changes in the concentration of substitution, less affected by temperature and pH. When there is a greater concentration of the solution is changed, the object will be released in a short time, for example, cyclodextrin complex will soon release the drug into the body after injection, the drug had little effect on the pharmacological. Cyclodextrin and guest molecules binding constants in 10-4M-1 at the time, reduced concentration sufficient to release the object. But for larger clathrate binding force, on concentration decreases, or no effect, replace a major competitive factor. Such as methanol, ethanol, and other small molecules can replace clathrate competitive object. The binding constant is determined by the nature of the cyclodextrin and the guest molecule, hydroxypropyl cyclodextrin cyclodextrin higher than the parent binding constant.

Products as a guest molecule by inclusion, the increased solubility, stability is improved, the liquid product can be powdered to prevent the volatile components evaporate, cover the drug bad smell or taste, adjust the release rate, improve the bioavailability of the product, reduce irritating and toxic side effects of drugs. Cyclodextrin formulation for use in cosmetics, can improve the raw material in cosmetic formulations system stabilization; makes adding the active ingredient in cosmetics is more stable; to make the configuration of the emulsion is more stable; so add in a stable volatile matter cosmetics species; increase the solubility of lipophilic substances in cosmetics. Hydroxypropyl cyclodextrin as a novel functional molecules, its research and applications will be subject to more and more attention.

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