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

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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.

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Data Availability

Not Applicable.

References

  1. Iacucci M, De Silva S, Ghosh S. Mesalazine in inflammatory bowel disease: A trendy topic once again? Can J Gastroenterol. 2010;24:127–33.

    Article  PubMed  PubMed Central  Google Scholar 

  2. Kouhpeikar H, Butler AE, Bamian F, Barreto GE, Majeed M, Sahebkar A. Curcumin as a therapeutic agent in leukemia. J Cell Physiol. 2019;234:12404–14.

    Article  CAS  PubMed  Google Scholar 

  3. J N, VSSR K, De A. Nanostructured lipid carrier (NLC): A promising drug delivery system. Glob. J Nanomed. 2017. https://doi.org/10.19080/GJN.2017.01.5.

  4. Ferreira M, Chaves LL, Lima SAC, Reis S. Optimization of nanostructured lipid carriers loaded with methotrexate: A tool for inflammatory and cancer therapy. Int J Pharm. 2015;492:65–72.

    Article  CAS  PubMed  Google Scholar 

  5. Makoni PA, Khamanga SM, Walker RB. Muco-adhesive clarithromycin-loaded nanostructured lipid carriers for ocular delivery: formulation, characterization, cytotoxicity and stability. J Drug Deliv Sci Technol. 2021. https://doi.org/10.1016/j.jddst.2020.102171.

  6. Xue X, Cao M, Ren L, Qian Y, Chen G. Preparation and optimization of rivaroxaban by self-nanoemulsifying drug delivery system (SNEDDS) for enhanced Oral bioavailability and no food effect. AAPS PharmSciTech. 2018;19:1847–59.

    Article  CAS  PubMed  Google Scholar 

  7. Corrie L, Gundaram R, Kukatil L. Formulation and evaluation of Cassia tora Phytosomal gel using central composite design. Recent Innov Chem Eng. 2021;14:347–57.

    Google Scholar 

  8. Pinto F, Barros D, Reis CP, Fonseca LP. Optimization of nanostructured lipid carriers loaded with retinoids by central composite design. J Mol Liq. 2019. https://doi.org/10.1016/j.molliq.2019.111468.

  9. Awasthi A, Kumar A, Kumar R, Vishwas S, Khursheed R, Kaur J, Corrie L, Kumar B, Gulati M, Kumar D, Kaushik M, Gupta G, Prasher P, Chellapan DK, Kumar AP, Dua K, Singh SK. RP-HPLC method development and validation for simultaneous estimation of mesalamine and curcumin in bulk form as well as nanostructured lipid carriers. S Afr J Bot. 2022. https://doi.org/10.1016/j.sajb.2022.05.044.

  10. Natarajan J, Sanapalli BKR, Bano M, Singh SK, Gulati M, Karri VVSR. Nanostructured lipid carriers of pioglitazone loaded collagen/chitosan composite scaffold for diabetic wound healing. Adv Wound Care. 2019;8:499–513.

    Article  Google Scholar 

  11. Sharaf M, Arif M, Khan S, Abdalla M, Shabana S, Chi Z, Liu C. Co-delivery of hesperidin and clarithromycin in a nanostructured lipid carrier for the eradication of Helicobacter pylori in vitro. Bioorg Chem. 2021. https://doi.org/10.1016/j.bioorg.2021.104896.

  12. Sun D, Guo S, Yang L, Wang Y, Wei X, Song S. Silicone elastomer gel impregnated with 20 ( S ) - protopanaxadiol-loaded nanostructured lipid carriers for ordered diabetic ulcer recovery. Acta Pharmacol Sin. 2020;41:119–28.

    Article  CAS  PubMed  Google Scholar 

  13. Hwang JH, Kim KJ, Ryu SJ, Lee BY. Caffeine prevents LPS-induced inflammatory responses in RAW264.7 cells and zebrafish. Chem Biol Interact. 2016;248:1–7.

    Article  CAS  PubMed  Google Scholar 

  14. Gardouh AR, Gad S, Ghonaim HM, Ghorab MM. Design and characterization of glyceryl monostearate solid lipid nanoparticles prepared by high shear homogenization. British J Pharm Research. 2013;3:326–46.

    Article  Google Scholar 

  15. Pizzol CD, Filippin-Monteiro FB, Restrepo JAS, Pittella F, Silva AH, de Souza PA, de Campos AM, Creczynski-Pasa TB. Influence of surfactant and lipid type on the physicochemical properties and biocompatibility of solid lipid nanoparticles. Int J Environ Res Public Health. 2014;11:8581–96.

    Article  PubMed  PubMed Central  Google Scholar 

  16. Elmowafy M, Al-Sanea MM. Nanostructured lipid carriers (NLCs) as drug delivery platform: advances in formulation and delivery strategies. Saudi Pharm J. 2021;29:999–1012.

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  17. Varshosaz J, Jandaghian S, Mirian M, Sajjadi SE. Co-delivery of rituximab targeted curcumin and imatinib nanostructured lipid carriers in non-Hodgkin lymphoma cells. J Liposome Res. 2021;31:64–78.

    Article  CAS  PubMed  Google Scholar 

  18. Rapalli VK, Kaul V, Waghule T, Gorantla S, Sharma S, Roy A, Dubey SK, Singhvi G. Curcumin loaded nanostructured lipid carriers for enhanced skin retained topical delivery: optimization, scale-up, in-vitro characterization and assessment of ex-vivo skin deposition. Eur J Pharm Scie. 2020;152:105438.

    Article  CAS  Google Scholar 

  19. Shah NV, Seth AK, Balaraman R, Aundhia CJ, Maheshwari RA, Parmar GR. Nanostructured lipid carriers for oral bioavailability enhancement of raloxifene: design and in vivo study. J Adv Res. 2016;7:423–34.

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  20. Kaur J, Gulati M, Famta P, Corrie L, Awasthi A, Saini S, Khatik GL, Bettada VG, Madhunapantula SRV, Paudel KR, Gupta G, Chellapan DK, Arshad MF, Admas J, Gowthamrajan K, Dua K, Hansbro PM, Singh SK. Polymeric micelles loaded with glyburide and vanillic acid: I. formulation development, in-vitro characterization and bioavailability studies. Int J Pharm. 2022. https://doi.org/10.1016/j.ijpharm.2022.121987.

  21. Khursheed R, Singh SK, Wadhwa S, Gulati M, Awasthi A, Kumar R, Ramanunny AK, Kapoor B, Kumar P, Corrie L. Exploring role of probiotics and Ganoderma lucidum extract powder as solid carriers to solidify liquid self-nanoemulsifying delivery systems loaded with curcumin. Carbohydr Polym. 2020. https://doi.org/10.1016/j.carbpol.2020.116996.

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Acknowledgements

Authors are thankful to Central Instrumentation Facility, Lovely Professional University for providing necessary support in terms of sample analysis using sophisticated instruments such as SEM and HPLC.

Funding

This research did not receive any specific grant from funding agencies in the public, commercial, or not-for-profit sectors.

Author information

Authors and Affiliations

Authors

Contributions

Authors’ Contributions

S.N.

Authors

CRediT role(s)

1

Ankit Awasthi

Methodology, Data Curation and Writing – original draft

2

Bimlesh Kumar

Supervision

3

Monica Gulati

Supervision

4

Sukriti Vishwas

Methodology

5

Leander Corrie

Methodology

6

Jaskiran Kaur

Methodology

7

Rubiya Khursheed

Methodology

8

Rozhan Arif Muhammed

Methodology

9

Duran Kala

Methodology

10

Omji Porwal

Methodology

11

Malakapogu Ravindra Babu

Methodology

12

M.V.N.L. Chaitanya

Methodology

13

Ankit Kumar

Methodology

14

Narendra Kumar Pandey

Methodology

15

Harish Dureja,

Review & editing

16

Dinesh Kumar Chellappan

Review & editing

17

Niraj Kumar Jha

Methodology

18

Gaurav Gupta

Methodology

19

Parteek Prasher

Methodology

20

Deepak Kumar

Methodology

21

Kamal Dua

Supervision

22

Sachin Kumar Singh

Conceptualization, Validation, Supervision, Review & editing

Corresponding author

Correspondence to Sachin Kumar Singh.

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Awasthi, A., Kumar, B., Gulati, M. et al. Novel Nanostructured Lipid Carriers Co-Loaded with Mesalamine and Curcumin: Formulation, Optimization and In Vitro Evaluation. Pharm Res 39, 2817–2829 (2022). https://doi.org/10.1007/s11095-022-03401-z

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

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