Cyclodextrins (CDs) have emerged as important encapsulation platforms in dermatologic and cosmetic sciences, addressing critical challenges related to the solubility and stability of bioactive compounds. This review (Part I) systematically explores the relationship between the molecular architecture of CDs and their functional performance at the skin interface. A comprehensive analysis of the physicochemical properties of natural and derivative cyclodextrins is presented, alongside an evaluation of their interaction mechanisms with the skin barrier and current regulatory frameworks. This study highlights how the hydrophobic cavity of CDs enables the successful encapsulation of botanical extracts, significantly enhancing their bioavailability and photostability. Furthermore, the mechanistic insights provided clarify how appropriately selected and formulated CDs can modulate skin penetration while maintaining acceptable epidermal barrier compatibility. A critical synthesis of safety data and toxicological profiles confirms the suitability of specific CD types for topical application, supported by an overview of the evolving European and international legislative landscapes. Understanding the molecular design and safety constraints of cyclodextrin-based systems is essential for developing next-generation dermocosmetics. This foundational analysis provides the necessary framework for the clinical and technological applications discussed in the subsequent part of this review.

Carvedilol (CARV) is a nonselective beta and alpha-1 adrenoceptor antagonist commonly indicated for chronic heart failure and hypertension. Its clinical potential is limited by its low aqueous solubility, resulting in poor bioavailability. Encapsulation of CARV by cyclodextrins (CDs) was performed to exceed its solubility-related barriers. This study examines the impact of the CD type and ethanol, as a co-solvent used in the preparation step, on the complexation of CARV with two β-CD derivatives. The inclusion complexes (ICs) were prepared employing the kneading method and investigated using different analytical techniques, including thermoanalytical methods, powder X-ray diffractometry (PXRD), universal attenuated total reflectance Fourier transform infrared (UATR-FTIR) spectroscopy, UV spectroscopy and saturation solubility studies. The binary products of CARV with heptakis(2,6-di-O-methyl)-β-cyclodextrin (DM-β-CD) and randomly methylated β-cyclodextrin (RM-β-CD) exhibit different thermal behavior, different FTIR spectral and diffractometric profiles from those of the parent compounds, emphasizing the interaction between the components and the IC formation. CARV solubility increased 1.78 to 3.32 times as a result of drug complexation with CDs. Analytical data indicate a significant influence of both solvent systems and CD type on the IC solubility, highlighting the CARV/DM-β-CD IC as a promising entity for further research to obtain new formulations containing CARV with improved bioavailability.

Carvedilol (CARV) belongs to the group of non-selective beta and alpha-1 adrenergic receptor antagonists and is indicated for hypertension and chronic heart failure