CATIONIC NANOSTRUCTURED LIPID CARRIERS: OPTIMIZATION OF ZETA POTENTIAL AND EVALUATION

MIRZA SALMAN BAIG; AQUIL-UR-RAHIM SIDDIQUI

doi:10.22159/ijap.2020v12i4.37531

Authors

MIRZA SALMAN BAIG Y. B. Chavan College of Pharmacy, Dr Babasaheb Ambedkar Marathwada University, Aurangabad, Maharashtra, India, Anjuman-i-Islam’s Kalsekar Technical Campus, School of Pharmacy, Affiliated to University of Mumbai, Maharashtra, India https://orcid.org/0000-0001-8220-8152
AQUIL-UR-RAHIM SIDDIQUI Shri Bhagwan College of Pharmacy, Dr Babasaheb Ambedkar Marathwada University, Aurangabad, Maharashtra, India

DOI:

https://doi.org/10.22159/ijap.2020v12i4.37531

Keywords:

SLN, NLC, CNLC, Cationic Nanostructured Lipid Carriers, Design-Expert, Ocular, Ophthalmic, Drug delivery, Nanoparticles, Cell uptake

Abstract

Objective: To fabricate, optimize and evaluate, Lipid-based cationic nanoparticulate dispersed system to improve the bio-adhesion property for ophthalmic use.

Methods: Lipid-based cationic nanoparticulate dispersed system was fabricated by melt emulsification ultrasonication method and Box-Behnken design was utilized for optimization of formulation through the Design-Expert® program. The concentration of stabilizer, liquid lipid and Cetyltrimethylammonium Bromide (CTAB) was selected as variables (factors) while particle size, zeta potential and polydispersity index (PDI) were selected as a response for optimization purpose. Characterization of particle properties was performed using Transmission Electron Microscopy (TEM), Photon correlation spectroscopy (PCS). Fourier-transform infrared spectroscopy (FT-IR) was performed to study chemical interaction among ingredients. Rhodamine B entrapped CNLC formulation was used to study the interaction of NLC and CNLC on a three-dimensional and two-dimensional ocular tissue model for cell uptake and penetration properties.

Results: Cationic nanostructured lipid carrier system was successfully fabricated by melt emulsification ultrasonication method. Characterization of nanoparticulate system using PCS revealed particle size in the range of 113.1 to 274.2 nm, PDI in a range of 0.147 to 0.280, while zeta potential in the range of 7.2 to 49.8 mV. The validation of statistical design suggested that it was suitable for navigation of design space. TEM imaging confirmed the results of PCS characterization. FT-IR study suggested a minimal chemical interaction among ingredients in CNLC. Confocal laser microscopic imaging for the interaction of NLC and CNLC on a three-dimensional and two-dimensional ocular tissue model revealed good penetration and bio-adhesion properties.

Conclusion: The fabricated Cationic nanostructured lipid carrier system was found to be the potential ophthalmic novel drug delivery system with good bio-adhesion and penetration properties.

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References

Sanchez Lopez E, Espina M, Doktorovova S, Souto EB, García ML. Lipid nanoparticles (SLN, NLC): Overcoming the anatomical and physiological barriers of the eye–part I–barriers and determining factors in ocular delivery. Eur J Pharm Biopharm 2017;110:70–5.

Sanchez Lopez E, Espina M, Doktorovova S, Souto EB, Garcia ML. Lipid nanoparticles (SLN, NLC): overcoming the anatomical and physiological barriers of the eye–part II-ocular drug-loaded lipid nanoparticles. Eur J Pharm Biopharm 2017;110:58–69.

Lang JC. Ocular drug delivery conventional ocular formulations. Adv Drug Delivery Rev 1995;16:39-43.

Dholakia M, Dave R, Thakkar V, Rana H, Gohel M, Patel N. Newer ophthalmic in situ gel of moxifloxacin hydrochloride: optimization using box behnken statistical design. Int J Pharm Pharm Sci 2018;10:5.

Niamprem P, Srinivas SP, Tiyaboonchai W. Development and characterization of indomethacin-loaded mucoadhesive nanostructured lipid carriers for topical ocular delivery. Int J Appl Pharm 2018;10:91–6.

Baig MS, Ahad A, Aslam M, Imam SS, Aqil M, Ali A. Application of box-behnken design for preparation of levofloxacin-loaded stearic acid solid lipid nanoparticles for ocular delivery: optimization, in vitro release, ocular tolerance, and antibacterial activity. Int J Biol Macromol 2016;85:258–70.

Das S, Ng WK, Tan RBH. Are nanostructured lipid carriers (NLCs) better than solid lipid nanoparticles (SLNs): development, characterizations and comparative evaluations of clotrimazole-loaded SLNs and NLCs? Eur J Pharm Sci 2012;47:139–51.

Liu R, Wang S, Sun L, Fang S, Wang J, Huang X, et al. A novel cationic nanostructured lipid carrier for improvement of ocular bioavailability: design, optimization, in vitro and in vivo evaluation. J Drug Delivery Sci Technol 2016;33:28–36.

Botto C, Mauro N, Amore E, Martorana E, Giammona G, Bondì ML. Surfactant effect on the physicochemical characteristics of cationic solid lipid nanoparticles. Int J Pharm 2017;516:334–41.

Fangueiro JF, Andreani T, Egea MA, Garcia ML, Souto SB, Silva AM, et al. Design of cationic lipid nanoparticles for ocular delivery: development, characterization and cytotoxicity. Int J Pharm 2014;461:64–73.

Oyewumi MO, Wehrung D, Sadana P. Gelucire-stabilized nanoparticles as a potential DNA delivery system. Pharm Dev Technol 2016;21:647–54.

Date AA, Vador N, Jagtap A, Nagarsenker MS. Lipid nanocarriers (GeluPearl) containing amphiphilic lipid gelucire 50/13 as a novel stabilizer: Fabrication, characterization and evaluation for oral drug delivery. Nanotechnology 2011;22:275102.

Baig MS, Owida H, Njoroge W, Siddiqui A ur R, Yang Y. Development and evaluation of cationic nanostructured lipid carriers for ophthalmic drug delivery of besifloxacin. J Drug Delivery Sci Technol 2020;55:101496.

Aslam M, Aqil M, Ahad A, Najmi AK, Sultana Y, Ali A. Application of Box-Behnken design for preparation of glibenclamide loaded lipid-based nanoparticles: optimization, in vitro skin permeation, drug release and in vivo pharmacokinetic study. J Mol Liq 2016;219:897–908.

Ameeduzzafar, Imam SS, Bukhari SNA, Ali A. Preparation and evaluation of novel chitosan: gelrite ocular system containing besifloxacin for topical treatment of bacterial conjunctivitis: scintigraphy, ocular irritation and retention assessment. Artif Cells Nanomed Biotechnol 2018;46:959–67.

Gardouh A, H Faheim S, M Solyman S. Design, optimization and in vitro evaluation of antifungal activity of nanostructured lipid carriers of tolnaftate. Int J Pharm Pharm Sci 2019;11:109–15.

Kumar S, Bhanjana G, Kumar A, Taneja K, Dilbaghi N, Kim KH. Synthesis and optimization of ceftriaxone-loaded solid lipid nanocarriers. Chem Phys Lipids 2016;200:126–32.

Hornof M, Toropainen E, Urtti A. Cell culture models of the ocular barriers. Eur J Pharm Biopharm 2005;60:207–25.

Gater R, Ipek T, Sadiq S, Nguyen D, Jones L, El Haj A, et al. Investigation of conjunctival fibrosis response using a 3D glaucoma tenon’s capsule+conjunctival model. Invest Ophthalmol Vis Sci 2019;60:605–14.

Moghddam SMM, Ahad A, Aqil M, Imam SS, Sultana Y. Optimization of nanostructured lipid carriers for topical delivery of nimesulide using box–behnken design approach. Artif Cells Nanomed Biotechnol 2017;45:617–24.

Gupta H, Aqil M, Khar RK, Ali A, Bhatnagar A, Mittal G. Sparfloxacin-loaded PLGA nanoparticles for sustained ocular drug delivery. Nanomed Nanotechnol Biol Med 2010;6:324–33.

Khan AM, Mehmood A, Sayed M, Nazar MF, Ismail B, Khan RA, et al. Influence of acids, bases and surfactants on the photocatalytic degradation of a model dye rhodamine B. J Mol Liq 2017;236:395–403.

Patil A, Lakhani P, Taskar P, Wu KW, Sweeney C, Avula B, et al. Formulation development, optimization, and in vitro–in vivo characterization of natamycin-loaded PEGylated nano-lipid carriers for ocular applications. J Pharm Sci 2018;107:2160-71.