Preformulation screening of lipids using solubility parameter concept in conjunction with experimental research to develop ceftriaxone loaded nanostructured lipid carriers
DOI:
https://doi.org/10.1590/s2175-97902023e21308Keywords:
PAMPA-PBL; X-ray diffraction; Imperfect crystalline; The full width half maximum; Solubility parameterAbstract
Development of ceftriaxone loaded nanostructured lipid carriers to increase permeability of ceftriaxone across uninflamed meninges after parenteral administration. Lipids were selected by theoretical and experimental techniques and optimization of NLCs done by response surface methodology using Box-Behnken design. The Δδt for glyceryl monostearate and Capryol90 were 4.39 and 2.92 respectively. The drug had maximum solubility of 0.175% (w/w) in glycerol monostearate and 2.56g of Capryol90 dissolved 10mg of drug. The binary mixture consisted of glyceryl monostearate and Capryol90 in a ratio of 70:30. The optimized NLCs particle size was 130.54nm, polydispersity index 0.28, % entrapment efficiency 44.32%, zeta potential -29.05mV, and % drug loading 8.10%. In vitro permeability of ceftriaxone loaded NLCs was 5.06x10-6 cm/s; evidently, the NLCs pervaded through uninflamed meninges, which, was further confirmed from in vivo biodistribution studies. The ratio of drug concentration between brain and plasma for ceftriaxone loaded NLCs was 0.29 and that for ceftriaxone solution was 0.02. With 44.32% entrapment of the drug in NLCs the biodistribution of ceftriaxone was enhanced 7.9 times compared with that of ceftriaxone solution. DSC and XRD studies revealed formation of imperfect crystalline NLCs. NLCs improved permeability of ceftriaxone through uninflamed meninges resulting in better management of CNS infections.
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Alam T, Pandit J, Vohora D, Aqil M, Ali A, Sultana Y. Optimization of nanostructured lipid carriers of lamotrigine for brain delivery: in vitro characterization and in vivo efficacy in epilepsy. Expert Opin Drug Del. 2015;12(2):181-94.
Almousallam M, Moia C, Zhu H. Development of nanostructured lipid carrier for dacarbazine delivery. Int Nano Lett. 2015;5(4):241-8.
Ameeduzzafar Z, Ibrahim El-Bagory, Alruwaili NK, Mohammed HE, Javed A, Muhammad A, et al. Development of novel dapagliflozin loaded solid self-nanoemulsifying oral delivery system: Physiochemical characterization and in vivo antidiabetic activity. J Drug Deliv Sci Tec. 2019;54:101279.
Ameeduzzafar Z, Qumber M, Alruwaili NK, Bukhari SNA, Alharbi KS, Imam SS, et al. BBD-Based development of itraconazole loaded nanostructured lipid carrier for topical delivery: in vitro evaluation and antimicrobial assessment. J Pharm Innov. 2021;16(3):85-98.
Ameeduzzafar Z. Development of oral lipid based nano-formulation of dapagliflozin: optimization, in vitro characterization and ex vivo intestinal permeation study. J Oleo Sci. 2020;69(11):1389-1401.
Barra J, Lescure F, Doelker E, Bustamante P. The expanded Hansen approach to solubility parameters. Paracetamol and citric acid in individual solvents. J Pharm Pharmacol. 1997;49(7):644-51.
Cherubin CE, Eng RH, Norrby R, Modai J, Humbert G, Overturf G. Penetration of newer cephalosporins into cerebrospinal fluid. Rev Infect Dis. 1989;11(4):526-48.
Eedara BB, Rangnekar B, Doyle C, Cavallaro A, Das SC. The influence of surface active l-leucine and 1, 2-dipalmitoyl-sn-glycero-3-phosphatidylcholine (DPPC) in the improvement of aerosolization of pyrazinamide and moxifloxacin co-spray dried powders. Int J Pharm. 2018;542(1-2):72-81.
Emmerson AM, Lamport PA, Reeves DS, Bywater MJ, Holt HA, Wise R, et al. The in vitro antibacterial activity of ceftriaxone in comparison with nine other antibiotics. Curr Med Res Opin. 1985;9(7):480-93.
Feng F, Zheng D, Zhang D, Duan C, Wang Y, Jia L, et al. Preparation, characterization and biodistribution of nanostructured lipid carriers for parenteral delivery of bifendate. J Microencapsul. 2011;28(4):280-5.
Gartziandia O, Herran E, Pedraz JL, Carro E, Igartua M, Hernandez RM. Chitosan coated nanostructured lipid carriers for brain delivery of proteins by intranasal administration. Colloid Surf B. 2015;134:304-13.
Gonzalo R, Laura TA, Fannyd’Orlyé, Anne V. Electrophoretic methods for characterizing nanoparticles and evaluating their bio-interactions for their further use as diagnostic, imaging, or therapeutic tools. Colin F. Poole, editor. In Handbooks in Separation Science, Capillary Electromigration Separation Methods. Elsevier. 2018;397-421.
Graverini G, Piazzini V, Landucci E, Pantano D, Nardiello P, Casamenti F, et al. Solid lipid nanoparticles for delivery of andrographolide across the blood-brain barrier: in vitro and in vivo evaluation. Colloid Surf B . 2018;161:302-13.
Hancock BC, York P, Rowe RC. The use of solubility parameters in pharmaceutical dosage form design. Int J Pharm . 1997;148(1):1-21.
Hansen CM. The three-dimensional solubility parameters-key to paint component affinities, solvents, plasticizers, polymers and resins. J Paint Technol. 1967;39:104-117.
Hao J, Fang X, Zhou Y, Wang J, Guo F, Li F, et al. Development and optimization of solid lipid nanoparticle formulation for ophthalmic delivery of chloramphenicol using a Box-Behnken design. Int J Nanomed. 2011;6:683-92.
Huttunen K, Rautio J. Prodrugs-an efficient way to breach delivery and targeting barriers. Curr Top Med Chem. 2011;(18):2265-87.
Jayanthi B, Sarojini S, Manikandan M, Manna PK. Application of central composite design based on response surface methodology for optimization of extended release aceclofenac microparticles. Eur J Pharm Med Res. 2016;3(10):163-172.
Kasongo KW, Müller RH, Walker RB. The use of hot and cold high pressure homogenization to enhance the loading capacity and encapsulation efficiency of nanostructured lipid carriers for the hydrophilic antiretroviral drug, didanosine for potential administration to paediatric patients. Pharm Dev Technol. 2012;17(3):353-62.
Kasongo WA, Pardeike J, Müller RH, Walker RB. Selection and characterization of suitable lipid excipients for use in the manufacture of didanosine-loaded solid lipid nanoparticles and nanostructured lipid carriers. J Pharm Sci. 2011;100(12):5185-96.
Kovacevic A, Savic S, Vuleta G, Mueller RH, Keck CM. Polyhydroxy surfactants for the formulation of lipid nanoparticles (SLN and NLC): effects on size, physical stability and particle matrix structure. Int J Pharm . 2011;406(1-2):163-72.
Krevelen DV. Cohesive properties and solubility. In: Properties and Polymers. 2009;189-225.
Lakshmi KS, Ilango K, Nithya MN, Balaji S, KibeVictor DW, Sathish KV. Spectrophotometric methods for the estimation of ceftriaxone sodium in vials. Int J Pharm Sci. 2009;1:22-5.
Li XW, Lin XH, Zheng LQ, Yu L, Mao HZ. Preparation, characterization, and in vitro release of chloramphenicol loaded solid lipid nanoparticles. J Disper Sci Technol. 2008;29(9):1214-21.
Li Y, Taulier N, Rauth AM, Wu XY. Screening of lipid carriers and characterization of drug-polymer-lipid interactions for the rational design of polymer-lipid hybrid nanoparticles (PLN). Pharm Res. 2006;23(8):1877-87.
Mahdi WA, Bukhari SI, Imam SS, Alshehri S, Zafar A, Yasir M. Formulation and optimization of butenafine-loaded topical nano lipid carrier-based gel: characterization, irritation study, and anti-fungal activity. Pharmaceutics. 2021;13(7):1087.
Mandell GL, Sande MA. Antimicrobial agents: penicillins, cephalosporins, and other beta-lactam antibiotics. Goodman & Gilman’s The pharmacologic basis of therapeutics, 9th ed. New York: McGraw-Hill, Health Professions Division. 1996:1073-101.
McDaid FM, Barker SA, Fitzpatrick S, Petts CR, Craig DQ. Further investigations into the use of high sensitivity differential scanning calorimetry as a means of predicting drug-excipient interactions. Int J Pharm . 2003;18;252(1-2):235-40.
Mohammed HE, Mohammed E, Khaled S, Ahmed FA, Naveed A, Ameeduzzafar Z, Hussein ME. Development and machine-learning optimization of mucoadhesive nanostructured lipid carriers loaded with fluconazole for treatment of oral candidiasis. Drug Dev Ind Pharm. 2021;47(2):246-258.
Nasiri M, Azadi A, Zanjani MRS, Hamidi M. Indinavir-loaded nanostructured lipid carriers to brain drug delivery: optimization, characterization and neuropharmacokinetic evaluation. Curr Drug Deliv. 2019;16(4):341-354.
Nau R, Prange HW, Muth P, Mahr G, Menck S, Kolenda H, et al. Passage of cefotaxime and ceftriaxone into cerebrospinal fluid of patients with uninflamed meninges. Antimicrob Agents Chemother. 1993;37(7):1518-24.
Neves AR, Queiroz JF, Reis S. Brain-targeted delivery of resveratrol using solid lipid nanoparticles functionalized with apolipoprotein E. J Nanobiotechnol. 2016;14(1):1-1.
Padhi S, Mazumder R, Bisth S. Development and application of lipid nanotechnology on infectious diseases of CNS-current scenario. Ind J Pharm Educ Res. 2019;53(3):355-65.
Pani NR, Nath LK, Acharya S, Bhuniya B. Application of DSC, IST, and FTIR study in the compatibility testing of nateglinide with different pharmaceutical excipients. J Therm Anal Calorim. 2012;108(1):219-26.
Park SY, Kang Z, Thapa P, Jin YS, Park JW, Lim HJ, et al. Development of sorafenib loaded nanoparticles to improve oral bioavailability using a quality by design approach. Int J Pharm . 2019;566:229-38.
Patil GB, Surana SJ. Fabrication and statistical optimization of surface engineered PLGA nanoparticles for naso-brain delivery of ropinirole hydrochloride: in-vitro-ex-vivo studies. J Biomat Sci-Polym E. 2013;24(15):1740-56.
Rowe R, Interaction of lubricants with microcrystalline cellulose and anhydrous lactose - a solubility parameter approach. Int J Pharm . 1998;41(3):223-226.
Salem DS, Sliem MA, El-Sesy M, Shouman SA, Badr Y. Improved chemo-photothermal therapy of hepatocellular carcinoma using chitosan-coated gold nanoparticles. J Photochem Photobiol B. 2018;182:92-99.
Salunkhe SS, Bhatia NM, Kawade VS, Bhatia MS. Development of lipid based nanoparticulate drug delivery systems and drug carrier complexes for delivery to brain. J Appl Pharm Sci. 2015;5(5):110-29.
Santaguida S, Janigro D, Hossain M, Oby E, Rapp E, Cucullo L. Side by side comparison between dynamic versus static models of blood-brain barrier in vitro: a permeability study. Brain Res. 2006;1109(1):1-3.
Shah A, Yameen MA, Fatima N, Murtaza G. Chemical synthesis of chitosan/silver nanocomposites films loaded with moxifloxacin: their characterization and potential antibacterial activity. Int J Pharm . 2019;561:19-34.
Shah M, Agrawal Y. High throughput screening: an in silico solubility parameter approach for lipids and solvents in SLN preparations. Pharm Dev Technol . 2013;18(3):582-90.
Shah M, Agrawal YK, Garala K, Ramkishan A. Solid lipid nanoparticles of a water-soluble drug, ciprofloxacin hydrochloride. Indian J Pharm Sci . 2012;74(5):434.
Subedi RK, Kang KW, Choi HK. Preparation and characterization of solid lipid nanoparticles loaded with doxorubicin. Eur J Pharm Sci . 2009;37(3-4):508-13.
Tajes M, Ramos-Fernández E, Weng-Jiang X, Bosch-Morato M, Guivernau B, Eraso-Pichot A, et al. The blood-brain barrier: structure, function and therapeutic approaches to cross it. Mol Membr Biol. 2014;31(5):152-67.
Tsai MJ, Wu PC, Huang YB, Chang JS, Lin CL, Tsai YH, et al. Baicalein loaded in tocol nanostructured lipid carriers (tocol NLCs) for enhanced stability and brain targeting. Int J Pharm . 2012;423(2):461-70.
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