EXPERIMENTAL DEVELOPMENT AND MOLECULAR DOCKING: NANOSTRUCTURED LIPID CARRIERS (NLCs) OF COENZYME Q10 USING STEARIC ACID AND DIFFERENT LIQUID LIPIDS AS LIPID MATRIX

Authors

  • NI LUH DEWI ARYANI Department of Pharmaceutics, Faculty of Pharmacy, Airlangga University, Surabaya, Indonesia, Department of Pharmaceutics, Faculty of Pharmacy, University of Surabaya, Surabaya, Indonesia
  • SISWANDONO Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Airlangga University, Surabaya, Indonesia
  • WIDJI SOERATRI Department of Pharmaceutics, Faculty of Pharmacy, Airlangga University, Surabaya, Indonesia
  • FANNY PUTRI RAHMASARI Department of Pharmaceutics, Faculty of Pharmacy, University of Surabaya, Surabaya, Indonesia
  • DIAN RIZKI KARTIKA SARI Department of Pharmaceutics, Faculty of Pharmacy, University of Surabaya, Surabaya, Indonesia

DOI:

https://doi.org/10.22159/ijap.2021v13i1.39890

Keywords:

Coenzyme Q10, Nanostructured lipid carriers, Stearic acid, Molecular docking

Abstract

Objective: To develop coenzyme Q10 (co-Q10) nanostructured lipid carriers (NLCs) using stearic acid (SA) and various liquid lipids with different lipophilicity as well as highlights the use of in silico studies for predicting and elucidating the interaction of drug-lipid used as carries in NLCs, at the molecular level.

Methods: The co-Q10 NLCs were prepared using SA as solid lipid and oleic acid (OA), isopropyl myristate (IPM), as well as isopropyl palmitate (IPP) as liquid lipids by the high shear homogenization method. Firstly, the formulas were optimized by the appropriate required HLB (rHLB). The optimized NLCs were characterized in the particle size, distribution of particle size, zeta potential, crystallinity behavior, Fourier transform infrared (FT-IR) spectra, morphology, entrapment efficiency (EE), drug loading (DL), and pH value. The interaction of drug-lipids in silico was studied using the AutoDock Vina program.

Results: The co-Q10 NLCs using SA and the various liquid lipid possessed the mean particle size, polydispersity index (PDI), zeta potential, EE, DL, and pH values were 180 to 350 nm,<0.5,<-30 mV, 83 to 88%, 10 to 11%, and 5.0 to 5.6, respectively. The EE and DL of co-Q10 NLCs increased with decreasing in binding energy (∆G) in silico.

Conclusion: The co-Q10 NLCs using SA as solid lipid and OA, IPM, as well as IPP as liquid lipids were developed successfully. Furthermore, in silico study by molecular docking is a potential approach in predicting and elucidating the interaction of drug-lipid in the development of NLCs formulation.

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References

Zaki NM. Strategies for oral delivery and mitochondrial targeting of CoQ10. Drug Delivery 2016;23:1868–81.

Korkmaz E, Gokce EH, Ozer O. Development and evaluation of coenzyme Q10 loaded solid lipid nanoparticle hydrogel for enhanced dermal delivery. Acta Pharm 2013;63:517–29.

Müller RH, Staufenbiel S, Keck C. Lipid nanoparticles (SLN, NLC) for innovative consumer care and household products. Househ Pers Care Today 2014;9:18–25.

Naseri N, Valizadeh H, Zakeri Milani P. Solid lipid nanoparticles and Nanostructured lipid carriers: Structure preparation and application. Adv Pharm Bull 2015;5:305–13.

Fang CL, A Al-Suwayeh S, Fang JY. Nanostructured lipid carriers (NLCs) for drug delivery and targeting. Recent Pat Nanotechnol 2012;7:41–55.

Keck CM, Baisaeng N, Durand P, Prost M, Meinke MC, Müller RH. Oil-enriched, ultra-small Nanostructured lipid carriers (usNLC): a novel delivery system based on flip-flop structure. Int J Pharm 2014;477:227–35.

Flavia D, Conrado M, Thallysson Carvalho B, Daniele M, Luciana N, Salvana C, et al. Polymorphism, crystallinity and hydrophilic-lipophilic balance (HLB) of cetearyl alcohol and cetyl alcohol as raw materials for solid lipid nanoparticles (SLN). ASP Nanotechnol 2018;1:52–60.

Rowe RC, Sheskey PJ, Quinn ME. editors. Handbook of pharmaceutical excipient. London: The Pharmaceutical Press; 2015.

Siswandono. editor. Kimia Medisinal 2. 2nd ed. Surabaya: Airlangga University Press; 2016.

Hathout RM, Metwally AA. Towards better modeling of drug-loading in solid lipid nanoparticles: molecular dynamics, docking experiments and gaussian processes machine learning. Eur J Pharm Biopharm 2016;108:262–8.

Xia Q, Wang H. Preparation and characterization of coenzyme Q10-loaded nanostructured lipid carries as delivery systems for cosmetic component. NSTI-Nanotech 2010;3:498–501.

Patrick G. Organic chemistry. 2nd ed. Vol. 53. London and New York: Bios Scientific Publishers; 2005.

Sopyan I, Fudholi A, Muchtaridi M, Sari IP. Co-crystallization: a tool to enhance solubility and dissolution rate of simvastatin. J Young Pharm 2017;9:183–6.

Sinko PJ. editor. Martin’s physical pharmacy and pharmaceutical sciences: physical chemical and biopharmaceutical principles in the pharmaceutical sciences: 6th ed. Philadelphia: Lippincott Williams and Wilkins; 2011.

Zulfakar MH, Chan LM, Rehman K, Wai LK, Heard CM. Coenzyme Q10-loaded fish oil-based bigel system: probing the delivery across porcine skin and possible interaction with fish oil fatty acids. AAPS PharmSciTech 2018;19:1116–23.

Tzachev CT, Svilenov HL. Lipid nanoparticles at the current stage and prospects-a review article. Int J Pharm Sci Rev Res 2013;18:103–15.

Shah R, Eldridge D, Palombo E, Harding I. Optimisation and stability assessment of solid lipid nanoparticles using particle size and zeta potential. J Phys Sci 2014;25:59–75.

Severino P, Andreani T, Macedo AS, Fangueiro JF, Santana MHA, Silva AM, et al. Current state-of-art and new trends on lipid nanoparticles (SLN and NLC) for oral drug delivery. J Drug Delivery 2012. DOI:10.1155/2012/750891.

Akbari J, Saeedi M, Morteza Semnani K, Rostamkalaei SS, Asadi M, Asare Addo K, et al. The design of naproxen solid lipid nanoparticles to target skin layers. Colloids Surf B 2016;145:626–33.

Danaei M, Dehghankhold M, Ataei S, Hasanzadeh Davarani F, Javanmard R, Dokhani A, et al. Impact of particle size and polydispersity index on the clinical applications of lipidic nanocarrier systems. Pharmaceutics 2018;10:1–17.

Pornputtapitak W, Pantakitcharoenkul J, Panpakdee R, Teeranachaideekul V, Sinchaipanid N. Development of γ-oryzanol rich extract from leum pua glutinous rice bran loaded NLCs for topical delivery. J Oleo Sci 2018;67:125–33.

Fernandes AV, Pydi CR, Verma R, Jose J, Kumar L. Design, preparation and in vitro characterizations of fluconazole loaded NLCs. Brazilian J Pharm Sci 2020;56:1–14.

Mahajan A, Kaur S. Design, formulation, and characterization of stearic acid-based solid lipid nanoparticles of candesartan cilexetil to augment its oral bioavailability. Asian J Pharm Clin Res 2018;11:344–50.

Hu FQ, Jiang SP, Du YZ, Yuan H, Ye YQ, Zeng S. Preparation and characterization of stearic acid NLCs by solvent diffusion method in an aqueous system. Colloids Surf B 2005;45:167–73.

Abdelmonem R, El Nabarawi MA, Attia AM, Teaimaa M. Ocular delivery of natamycin solid lipid nanoparticle loaded mucoadhesive gel: formulation, characterization and in vivo study. Int J Appl Pharm 2020;12:173–80.

Keivani Nahr F, Ghanbarzadeh B, Samadi Kafil H, Hamishehkar H, Hoseini M. The colloidal and release properties of cardamom oil encapsulated NLC. J Dispers Sci Technol 2019;1–9. https://doi.org/10.1080/01932691.2019.1658597

Chauhan I, Mohd Y, Madhu V, SinghPratap A. NLCs: a groundbreaking approach for transdermal drug delivery. J Cardiovasc Thorac Res 2015;7:113–7.

Chen PC, Huang JW, Pang J. An investigation of optimum NLC-sunscreen formulation using taguchi analysis. J Nanomater 2013:7–12. https://doi.org/10.1155/2013/463732

Siafaka P, Okur ME, Ayla S, Er S, Caglar ES, Okur NU. Design and characterization of nanocarriers loaded with levofloxacin for enhanced antimicrobial activity; physicochemical properties, in vitro release and oral acute toxicity. Brazilian J Pharm Sci 2019;55:1–13.

Remya PN, Damodharan N. Formulation, development, and characterisation of nimodipine loaded solid lipid nanoparticles. Int J Appl Pharm 2020;12:265–71.

Korting MSHC. The pH of the skin surface and its impact on the barrier function. Ski Pharmacol Physiol 2006;19:296–302.

Geetha P, Sivaram AJ, Jayakumar R, Gopi Mohan C. Integration of in silico modeling, prediction by ∆Gand experimental approach to study the amorphous chitin nanocarriers for cancer drug delivery. Carbohydr Polym 2016;142:240–9.

Published

07-01-2021

How to Cite

ARYANI, N. L. D., SISWANDONO, SOERATRI, W., RAHMASARI, F. P., & SARI, D. R. K. (2021). EXPERIMENTAL DEVELOPMENT AND MOLECULAR DOCKING: NANOSTRUCTURED LIPID CARRIERS (NLCs) OF COENZYME Q10 USING STEARIC ACID AND DIFFERENT LIQUID LIPIDS AS LIPID MATRIX. International Journal of Applied Pharmaceutics, 13(1), 108–116. https://doi.org/10.22159/ijap.2021v13i1.39890

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