Enhancing ketoprofen's solubility and anti-inflammatory efficacy with safe methyl-β-cyclodextrin complexation

被引：5

作者：

Rajamohan, Rajaram ^{[1
]}

Kamaraj, Eswaran ^{[1
]}

Muthuraja, Perumal ^{[1
]}

Murugavel, Kuppusamy ^{[2
]}

Govindasamy, Chandramohan ^{[3
]}

Prabakaran, D. S. ^{[4
,5
]}

Malik, Tabarak ^{[6
,7
]}

Lee, Yong Rok ^{[1
]}

机构：

[1] Yeungnam Univ, Sch Chem Engn, Gyongsan 38541, South Korea

[2] Govt Arts Coll, PG & Res Dept Chem, Chidambaram 608 102, Tamil Nadu, India

[3] King Saud Univ, Coll Appl Med Sci, Dept Community Hlth Sci, POB 10219, Riyadh 11433, Saudi Arabia

[4] Chungbuk Natl Univ, Coll Med, Dept Radiat Oncol, Cheongju 28644, South Korea

[5] SRM Inst Sci & Technol, Sch Bioengn, Dept Biotechnol, Chennai 603203, Tamil Nadu, India

[6] Jimma Univ, Inst Hlth, Dept Biomed Sci, Jimma, Ethiopia

[7] Lovely Profess Univ, Div Res & Dev, Phagwara 144411, India

来源：

SCIENTIFIC REPORTS | 2024年 / 14卷 / 01期

关键词：

Ketoprofen; Methyl-beta-cyclodextrin; Inclusion complexation; Solubility enhancement; Apoptosis by cell cycle analysis; Anti-inflammation; INCLUSION COMPLEX; IN-VITRO; BENZYL ISOTHIOCYANATE; PHASE SOLUBILITY; ACID; BIOAVAILABILITY; DISSOLUTION; DRUG; PHOTOSTABILITY; ENCAPSULATION;

D O I：

10.1038/s41598-024-71615-9

中图分类号：

O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];

学科分类号：

07 ; 0710 ; 09 ;

摘要：

Improved solubility and anti-inflammatory (AI) properties are imperative for enhancing the effectiveness of poorly water-soluble drugs, particularly non-steroidal anti-inflammatory drugs (NSAIDs). To address these critical issues, our focus is on obtaining NSAID materials in the form of inclusion complexes (IC) with methyl-beta-cyclodextrin (MCD). Ketoprofen (KTP) is selected as the NSAID for this study due to its potency in treating various types of pain, inflammation, and arthritis. Our objective is to tackle the solubility challenge followed by enhancing the AI activity. Confirmation of complexation is achieved through observing changes in the absorbance and fluorescence intensities of KTP upon the addition of MCD, indicating a 1:1 stoichiometric ratio. Phase solubility studies demonstrated improved dissolution rates after the formation of ICs. Further analysis of the optimized IC is conducted using FT-IR, NMR, FE-SEM, and TG/DTA techniques. Notable shifts in chemical shift values and morphological alterations on the surface of the ICs are observed compared to their free form. Most significantly, the IC exhibited superior AI and anti-arthritic (AA) activity compared to KTP alone. These findings highlight the potential of ICs in expanding the application of KTP, particularly in pharmaceuticals, where enhanced stability and efficacy of natural AIs and AAs are paramount.

引用

页数：15