Novel Nanostructured Lipid Carriers Co-Loaded with Mesalamine and Curcumin: Formulation, Optimization and In Vitro Evaluation.

Rozhan Arif Muhammed, Sachin Kumar Singh, Kamal Dua, Deepak Kumar, Gaurav Gupta, Niraj Kumar Jha, Harish Dureja, M V N L Chaitanya, Malakapogu Ravindra Babu, Omji Porwal, Duran Kala, Dinesh Kumar Chellappan, Monica Gulati, Parteek Prasher, Ankit Kumar, Narendra Kumar Pandey, Bimlesh Kumar, Jaskiran Kaur, Rubiya Khursheed, Leander Corrie, Sukriti Vishwas, Ankit Awasthi

Journal: Pharmaceutical research 2022;39(11):2817-2829

PMID: 36195824

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Abstract

PURPOSE

The aim of current study is to formulate, optimize and characterize the developed formulation of Mesalamine-Curcumin Nanostructured Lipid Carriers (Mes-Cur NLCs).

METHODS

It was formulated using high pressure homogenization followed by probe sonication and formulation variables were optimized using Central Composite Design. The particle size (PS), zeta potential (ZP), entrapment efficiency (EE), drug release, cytotoxicity on NIH 3T3 fibroblasts cells and HaCaT keratinocytes cells and efficacy on RAW264.7 cells for optimized formulation was determined.

RESULTS

The PS, ZP and EE were found to be 85.26 nm, -23.7 ± 7.45 mV, 99.2 ± 2.62 % (Mes) and 84 ± 1.51 % (Cur), respectively. The good correlation between predicted and obtained value indicated suitability and reproducibility of experimental design. NLCs showed spherical shape as confirmed by TEM. In vitro drug release profile of prepared formulation showed that Mes exhibited 100 % release at 48 h, whereas Cur exhibited 82.23 ± 2.97% release at 120 h. Both the drugs exhibited sustained release upon incorporation into the NLCs. The absence of any significant cell death during MTT assay performed on NIH 3T3 fibroblasts cells and HaCaT keratinocytes cells indicated that NLCs' were safe for use. Furthermore, significant reduction in nitric oxide level during anti-inflammatory evaluation of formulation on RAW264.7 cells showed excellent potential for the formulation to treat inflammation. The formulation was found stable as no significant difference between the PS, ZP and EE of the fresh and aged NLCs was observed.

CONCLUSION

The outcomes of study deciphered successful formulation of Mes-Cur NLCs.

Address: School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, 144411, India.; Faculty of Health, Australian Research Centre in Complementary and Integrative Medicine, University of Technology Sydney, Ultimo, NSW, 2007, Australia.; Department of Pharmacognosy, Faculty of Pharmacy, Tishk International University-44001, Erbil, Kurdistan Region, Iraq.; Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, Haryana, 124001, India.; Department of Life Sciences, School of Pharmacy, International Medical University, Bukit Jalil, 57000, Kuala Lumpur, Malaysia.; Department of Biotechnology, School of Engineering & Technology (SET), Sharda University, Plot No.32-34 Knowledge Park III, Greater Noida, Uttar Pradesh, 201310, India.; School of Pharmacy, Suresh Gyan Vihar University, Mahal Road, Jagatpura, Jaipur, India.; Department of Pharmacology, Saveetha Dental College and Hospitals, Saveetha Institute of Medical and Technical Sciences, Saveetha University, Chennai, India.; Uttaranchal Institute of Pharmaceutical Sciences, Uttaranchal University, Dehradun, India.; Department of Chemistry, University of Petroleum & Energy Studies, Energy Acres, Dehradun, 248007, India.; Department of Pharmaceutical Chemistry, School of Pharmaceutical Sciences, Shoolini University, Solan, 173229, India.; Discipline of Pharmacy, Graduate School of Health, University of Technology Sydney, Sydney, Ultimo, NSW, 2007, Australia.; School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, 144411, India. [email protected].; Faculty of Health, Australian Research Centre in Complementary and Integrative Medicine, University of Technology Sydney, Ultimo, NSW, 2007, Australia. [email protected].

DOI: 10.1007/s11095-022-03401-z

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https://doi.org/10.1007/s11095-022-03401-z

MeSH Terms: Curcumin, Drug Carriers, Mesalamine, Lipids, Reproducibility of Results, Nanostructures, Particle Size