Review Article CYCLODEXTRIN AS SOLUBILIZER AND TARGETING AGENT FOR DRUGS ADITYA NARAYAN SINGH 1 , DILEEP SINGH BAGHEL 1 , BIMLESH KUMAR 1 , NARENDRA KUMAR PANDEY 1 , SAURABH SINGH 1 , KALVATALA SUDHAKAR 1* , R. NARAYANA CHARYULU 2 1 School of Pharmaceutical Sciences, lovely Professional University, Punjab, 144001, India. 2 Department of Pharmaceutics, NGSM Institute of Pharmaceutical Sciences, Nitte (Deemed to be University), Mangaluru-575018, India * Corresponding author: Kalvatala Sudhakar; * Email: ckbhaipharma@gmail.com Received: 31 Jan 2024, Revised and Accepted: 11 Jun 2024 ABSTRACT Natural cyclic oligosaccharides called cyclodextrins (CDs) improve the bioavailability of drugs by the formation of inclusion complexes involving small and macromolecules of poorly soluble compounds in water. CDs act as a solubilizer and targeting agent for drugs with low water solubility, enabling them to effectively target specific cells. Where poorly water-soluble compounds interact with the hydrophobic cavity of CDs to enhance their solubility. CDs are effective drug delivery agents because of their essential function as processing complex carriers. Various ligands can be utilized to modify the surface of cyclodextrin to actively target drugs. It is possible to consider it to have amphiphilic characteristics by enduring a chemical transformation with long aliphatic chains, and a variety of amphiphilic CDs can produce nanoparticles without the usage of surfactants. CD-nanocarriersact as cargo with solubilizers for drugs and a targeting agent for specific receptors present in specific cells and release the drug. CDs have many applications, including the reduction of drug-induced gastrointestinal discomfort, avoiding interactions between drug-drug and drug- excipient, and transforming drug products that are liquid into microcrystalline solid powders. Because of their biocompatibility and biodegradability, CDs have outstanding properties that make them particularly useful in the pharmaceutical and cosmetic industries. Keywords: Cyclodextrins, Inclusion complex, Solubilizer, Targeting agent, Nanoparticle, Nanocarrier © 2024 The Authors. Published by Innovare Academic Sciences Pvt Ltd. This is an open access article under the CC BY license (https://creativecommons.org/licenses/by/4.0/) DOI: https://dx.doi.org/10.22159/ijap.2024v16i4.50469 Journal homepage: https://innovareacademics.in/journals/index.php/ijap INTRODUCTION Cyclodextrins (CDs) are the products of the starch breakdown performed by the enzyme glucosyl transferase [1]. The articles for the current review were sourced from specialized databases.(Range of years: 2000-2024) such as Elsevier, Pubmed, and Ovid using the keywords Cyclodextrin Solubilty. Other selections include articles from Springer, information from Internet sources, and Online published articles from Nature Medscape. Google Scholar may be a viable addition as a search option for cyclodextrin searches. CDs are cyclic oligosaccharides that occur naturally and resemble a cone in their shape. On the inside of the cavity, they show hydrophobic characteristics and have a hydrophobic coating on the outside [2]. It is possible to increase the bioavailability of drugs by utilizing cyclodextrins that are soluble in water [3]. This is accomplished by forming inclusion complexes with sections of large compounds and tiny molecules that have poor aqueous solubility [4]. Hydrophobic interactions inside cavity-containing molecules, such as in aqueous solutions CDs, can significantly enhance the solubility of drugs. The resulting drug is both chemically and physiologically accessible [5]. Patients can be given pharmaceutical drugs that aren't very water- soluble or chemically stable using CDs. This makes it possible for more drugs to be given to patients [6]. As a consequence of this, CDs have the potential to convert molecules that possess biological activity but do not have the physiochemical features of drugs into drugs that have the required therapeutic effect [7]. CDs take on the role of hosts by allowing a portion of a drug molecule to be placed inside their core cavities to facilitate drug-containing inclusion complex formation [8]. Because of this modification, the Drugs’ physiochemical characteristics will be altered. For instance, by generating a Drug-CD inclusion complex, the product's aqueous solubility, physical and chemical stability, and distribution of the drug across biological membranes may all be enhanced [9]. During the process of complex formation, there is no creation or destruction of covalent bonds, and the drug particles that are bound inside the CD inclusion complex are present in a dynamic equilibrium with the drug compounds that are free in aqueous solutions [10] [fig. 1]. Fig. 1: Bucket shape CD forms inclusion complex In recent years, a strategy that is possible for the development of unique, optimized systems is the combination of CD derivatives [fig. 2] with nanomaterials. This technique has emerged as an affordable option [11]. It has been illustrated in research that CDs can reduce the toxicity of various drugs and be biologically compatible when compared to other pharmaceutical excipients. For this reason, they have the potential as components in new drug compositions, including the modification of current medicinal products [12, 13]. Cyclodextrin acts as a solubilizer CDs are practical functional excipients that have grabbed a lot of interest and are frequently used [14]. The pharmacological perspective is based on the ability of these components the interact with weakly water-soluble drugs and drug molecules, resulting in an enhancement in their apparent water solubility [15]. The capability of CDs to develop dynamic inclusion complexes formed through non- International Journal of Applied Pharmaceutics ISSN- 0975-7058 Vol 16, Issue 4, 2024