Formulation of Ensulizole with Beta-Cyclodextrins for Improved Sunscreen Activity and Biocompatibility

Rajaram Rajamohan; Eswaran Kamaraj; Chandramohan Govindasamy; Sivakumar Allur Subramanian; Sung Jae Kim; Mani Murali Krishnan; Kuppusamy Murugavel; Moorthiraman Murugan; Yong Rok Lee

doi:10.1016/j.xphs.2023.12.019

Formulation of Ensulizole with Beta-Cyclodextrins for Improved Sunscreen Activity and Biocompatibility

J Pharm Sci. 2023 Dec 24:S0022-3549(23)00546-4. doi: 10.1016/j.xphs.2023.12.019. Online ahead of print.

Authors

Rajaram Rajamohan¹, Eswaran Kamaraj², Chandramohan Govindasamy³, Sivakumar Allur Subramanian⁴, Sung Jae Kim⁴, Mani Murali Krishnan⁵, Kuppusamy Murugavel⁶, Moorthiraman Murugan⁷, Yong Rok Lee⁸

Affiliations

¹ School of Chemical Engineering, Yeungnam University, Gyeongsan 38541, Republic of Korea. Electronic address: rajmohanau@yu.ac.kr.
² School of Chemical Engineering, Yeungnam University, Gyeongsan 38541, Republic of Korea.
³ Department of Community Health Sciences, College of Applied Medical Sciences, King Saud University, P.O. Box 10219, Riyadh 11433, Saudi Arabia.
⁴ Department of Orthopaedic Surgery, Dongtan Sacred Heart Hospital, Hallym University, College of Medicine, Hwaseong, Republic of Korea.
⁵ Department of Chemistry, Bannari Amman Institute of Technology, Sathyamangalam 638 401, Tamil Nadu, India.
⁶ PG and Research Department of Chemistry, Government Arts College, Chidambaram 608 102, Tamil Nadu, India.
⁷ Department of Chemistry, IFET College of Engineering, Villupuram 605 108, Tamil Nadu, India.
⁸ School of Chemical Engineering, Yeungnam University, Gyeongsan 38541, Republic of Korea. Electronic address: yrlee@yu.ac.kr.

PMID: 38147911
DOI: 10.1016/j.xphs.2023.12.019

Abstract

In today's context, prolonged exposure to sunlight is widely recognized as a threat to human health, leading to a range of adverse consequences, including skin cancers, premature skin aging, and erythema. To mitigate these risks, preventive actions mainly focus on advocating the application of sunscreen lotions and minimizing direct exposure to sunlight. This research study specifically centered on ensulizole (ENS), a prominent ingredient in sunscreens. The objective was to create inclusion complexes (ICs) with Beta-cyclodextrin (B-CD) and its hydroxypropyl derivatives (H-CD). Using phase solubility measurements, we determined that both B-CD and H-CD form 1:1 stoichiometric ICs with ENS. Proton nuclear magnetic resonance spectral (¹H NMR) analysis confirmed that the phenyl portion of ENS is encapsulated within the B-CD cavity. Significant changes in surface morphology were observed during the formation of these ICs compared to ENS and CDs alone. Quantum mechanical calculations were employed to further support the formation of ICs by providing energy data. Particularly, the photostability of the ENS:B-CD ICs remained intact for up to four hours of UV exposure, with no significant alterations in the structure of ENS. Furthermore, comprehensive biocompatibility assessments yielded encouraging results, suggesting the potential application of these inclusion complexes in cosmetics as a UVB sunscreen. In summary, our research underscores the successful creation of inclusion complexes characterized by enhanced photostability and safe biocompatibility.

Keywords: Beta-cyclodextrins; Biocompatibility; Ensulizole; Improved sunscreen activity; Skin fibroblast cells.