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Cycloaddition Reactions: Overview01:16

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Cycloadditions are one of the most valuable and effective synthesis routes to form cyclic compounds. These are concerted pericyclic reactions between two unsaturated compounds resulting in a cyclic product with two new σ bonds formed at the expense of π bonds. The [4 + 2] cycloaddition, known as the Diels–Alder reaction, is the most common. The other example is a [2 + 2] cycloaddition.
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An Overview of Recent Patents and Future Perspective Based on Cyclodextrin Complexation.

Ritu Kaushik1, Ravinder Verma2, Vikas Budhwar1

  • 1Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak-124001, India.

Recent Advances in Drug Delivery and Formulation
|February 3, 2023
PubMed
Summary

Cyclodextrins (CDs) enhance the solubility and bioavailability of poorly water-soluble drugs. These pharmaceutical adjuvants improve drug stability and formulation, offering solutions for drug delivery challenges.

Keywords:
CDadvantage of α-CDcaptisolinclusion complexesmodified CDpatented technologiesβ-CDγ -CD

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery
  • Materials Science

Background:

  • Many orally administered drugs suffer from poor aqueous solubility and dissolution rates, limiting their bioavailability.
  • Poorly water-soluble (PWS) drugs present significant challenges in pharmaceutical formulation and development.
  • Cyclodextrins (CDs) are versatile pharmaceutical excipients that can address these solubility and bioavailability issues.

Purpose of the Study:

  • To provide a comprehensive overview of cyclodextrins (CDs) and their derivatives.
  • To discuss the manufacturing processes, physicochemical properties, and advantages of CDs in drug formulations.
  • To highlight recent advancements, patents, and specific examples of modified CDs in pharmaceutical applications.

Main Methods:

  • Review of scientific literature on cyclodextrins and their applications in drug delivery.
  • Analysis of the physicochemical properties and structural features of various cyclodextrin derivatives.
  • Examination of case studies and patented formulations utilizing cyclodextrin technology.

Main Results:

  • CDs form inclusion complexes with poorly water-soluble drugs, significantly enhancing their solubility, dissolution rate, and bioavailability.
  • CD-based formulations demonstrate improved drug stability, reduced drug irritation, and can act as taste and odor masking agents.
  • Various chemically modified CDs, including Captisol, sulfobutyl ether-β-CD, and hydroxy propyl betadex, are effectively used in diverse oral and parenteral dosage forms.

Conclusions:

  • Cyclodextrins and their derivatives are crucial pharmaceutical adjuvants for developing effective formulations of poorly water-soluble drugs.
  • CD technology offers a robust strategy to overcome drug delivery challenges, improving therapeutic efficacy and patient compliance.
  • The continuous development of novel cyclodextrin derivatives promises further advancements in pharmaceutical formulation and drug product innovation.