Introduction

By enclosing a different molecule of the right size and shape inside the spatial structure of one other molecule, inclusion complexes are a specific kind of molecular complex. The inclusion of the compound is also referred to as molecular capsules because it typically consists of two parts: Host material: able to form a specific cage, pipe or layer space, and can accommodate other material molecules of the main material. Host material can be a single molecule, can also be a multi-molecule lattice. Guest material: encapsulated in the inclusion compound. Therefore, the inclusion compound is also known as molecular capsules.

Importance of Inclusion Compounds

Solubility Enhancement: Inclusion compounds can significantly improve the solubility of poorly soluble APIs by providing an environment that promotes their dispersibility and dissolution in biological fluids, ultimately enhancing drug absorption and bioavailability.

Stability Improvement: By encapsulating APIs within inclusion complexes, stability issues such as degradation, oxidation, and hydrolysis can be mitigated or prevented, ensuring the integrity and efficacy of the drug during storage and administration.

Controlled Release: Inclusion compounds enable precise control over drug release kinetics, allowing for sustained, targeted, and site-specific delivery of APIs, thereby optimizing therapeutic outcomes and reducing dosing frequency.

Examples of Inclusion Compounds

Cyclodextrin Complexes

Cyclodextrins, such as β-cyclodextrin (β-CD), are widely used carriers for inclusion complexes. They are cyclic oligosaccharides with a hydrophobic cavity capable of encapsulating various hydrophobic drugs. For example, inclusion of poorly soluble drugs like itraconazole within β-cyclodextrin can enhance their solubility and oral bioavailability.

Zeolite Inclusion Compounds

Zeolites are crystalline, microporous materials with well-defined pore structures. They can be used as carriers to create inclusion compounds with a wide range of drugs, including small molecules, proteins, and peptides. Zeolite-based inclusion compounds offer improved drug stability and release properties. An example includes zeolite-encapsulated ibuprofen for sustained release applications.

Polymers

Certain polymers, such as polyvinylpyrrolidone (PVP) or polyethylene glycol (PEG), can form inclusion compounds with APIs. These polymer-based inclusion complexes provide enhanced solubility, stability, and controlled release capabilities. For instance, PVP inclusion complexes have been used to improve the dissolution rate and bioavailability of poorly soluble drugs like carbamazepine.

Applications in Different Dosage Formulations

Solid Dosage Forms

Inclusion compounds find widespread application in solid dosage forms such as tablets and capsules. They can enhance the solubility of APIs, improve their stability, and enable controlled release profiles. This is particularly beneficial for drugs with low aqueous solubility or those prone to degradation.

Parenteral Formulations

Pharmaceutical inclusion compounds can be utilized in parenteral formulations, including injectables and implants. The enhanced solubility and stability offered by these complexes facilitate better drug absorption and sustained release, ensuring optimal therapeutic efficacy.

Topical and Transdermal Preparations

Inclusion compounds can be incorporated into topical formulations, creams, gels, or transdermal patches. These complexes enhance the solubility of APIs, facilitate their penetration through the skin, and improve localized drug delivery for dermatological or localized applications.

Conclusion

Inclusion compounds provide a promising avenue for overcoming solubility and stability challenges in drug development. By harnessing the power of inclusion complexes, our company strives to offer comprehensive solutions that enhance drug delivery, ensuring improved bioavailability and therapeutic outcomes across various dosage forms. Partnering with Protheragen-ING, a reputable supplier, ensures the availability of high-quality excipients and supports the development of stable and efficacious pharmaceutical products. If you have any excipient requirements, please contact us by phone or email, and we will respond within 2-4 working days.