High payload dexamethasone palmitate-loaded solid lipid nanoparticles for enhanced anti-inflammatory effects in acute skin inflammation model
Tóm tắt
Dexamethasone palmitate (DXPL) is a lipophilic derivative of dexamethasone (DXM) used to overcome the low drug-loading capacity and immediate release characteristics of DXM from nanoparticles. In this study, we investigated the potential of DXPL-loaded solid lipid nanoparticles (DXPL-SLNs) to increase drug encapsulation efficiency, prolong drug release, and alleviate skin inflammation. DXPL-SLNs were prepared using the nano-emulsion template technique with trilaurin as a lipid matrix and Tween 20, Span 20, and Brij 58 as a surfactant mixture. The physicochemical properties of DXPL-SLNs were examined in terms of particle size, polydispersity index, zeta potential, encapsulation efficiency, loading capacity, morphology, and crystalline behavior. The in vitro release profile of DXM from the DXPL-SLNs incubated in mouse plasma was assessed using a plasma conversion assay. In vivo anti-inflammatory effects of topically applied DXPL-SLNs were evaluated in mice with 12-O-tetradecanoyl-phorbol-13-acetate (TPA)-induced ear edema. The optimized DXPL-SLNs (DXPL/trilaurin/Tween 20/Span 20/Brij 58:4/2/2/0.2/4, w/w ratio, respectively) displayed a mean particle size of 182.8 ± 2.7 nm with a very high drug loading capacity of 30.4%. DXPL-SLNs showed substantially prolonged drug release in mouse plasma compared to DXPL solution. Furthermore, DXPL-SLNs showed enhanced anti-inflammatory effects by efficiently reducing TPA-induced ear edema. These findings suggest that DXPL-SLNs have great potential as anti-inflammatory therapeutics against acute skin inflammation.
Từ khóa
Tài liệu tham khảo
Akram M, Shin I, Kim K-A, Noh D, Baek S-H, Chang S-Y, Kim H, Bae O-N (2016) A newly synthesized macakurzin C-derivative attenuates acute and chronic skin inflammation: the Nrf2/heme oxygenase signaling as a potential target. Toxicol Appl Pharmacol 307:62–71
Andújar I, Recio M, Bacelli T, Giner R, Ríos J (2010) Shikonin reduces oedema induced by phorbol ester by interfering with IκBα degradation thus inhibiting translocation of NF-κB to the nucleus. Br J Pharmacol 160:376–388
Bralley EE, Greenspan P, Hargrove JL, Wicker L, Hartle DK (2008) Topical anti-inflammatory activity of Polygonum cuspidatum extract in the TPA model of mouse ear inflammation. J Inflamm 5:1
Cai Y, Xu H, Yan J, Zhang L, Lu Y (2014) Molecular targets and mechanism of action of dexmedetomidine in treatment of ischemia/reperfusion injury. Mol Med Rep 9:1542–1550
Cruz-Topete D, Cidlowski JA (2015) One hormone, two actions: anti- and pro-inflammatory effects of glucocorticoids. Neuroimmunomodulation 22:20–32
Das S, Ng WK, Kanaujia P, Kim S, Tan RB (2011) Formulation design, preparation and physicochemical characterizations of solid lipid nanoparticles containing a hydrophobic drug: effects of process variables. Colloids Surf B: Biointerfaces 88:483–489
Das S, Ng WK, Tan RBH (2012) 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 47:139–151
Doi M, Ishida T, Sugio S, Imagawa T, Inoue M (1989) Physicochemical properties of dexamethasone palmitate, a high fatty acid ester of an anti-inflammatory drug: polymorphism and crystal structure. J Pharm Sci 78:417–422
Dudhipala N, Veerabrahma K (2017) Improved anti-hyperlipidemic activity of Rosuvastatin Calcium via lipid nanoparticles: pharmacokinetic and pharmacodynamic evaluation. Eur J Pharm Biopharm 110:47–57
Gómez-Gaete C, Fattal E, Silva L, Besnard M, Tsapis N (2008) Dexamethasone acetate encapsulation into Trojan particles. J Control Release 128:41–49
Gómez-Gaete C, Tsapis N, Besnard M, Bochot A, Fattal E (2007) Encapsulation of dexamethasone into biodegradable polymeric nanoparticles. Int J Pharm 331:153–159
Graverini G, Piazzini V, Landucci E, Pantano D, Nardiello P, Casamenti F, Pellegrini-Giampietro DE, Bilia AR, Bergonzi MC (2018) Solid lipid nanoparticles for delivery of andrographolide across the blood-brain barrier: in vitro and in vivo evaluation. Colloids Surf B: Biointerfaces 161:302–313
Gul M, Shah FA, Sahar N-u, Malik I, Din Fu, Khan SA, Aman W, Choi H-I, Lim C-W, Noh H-Y, Noh J-S, Zeb A, Kim J-K (2022) Formulation optimization, in vitro and in vivo evaluation of agomelatine-loaded nanostructured lipid carriers for augmented antidepressant effects. Colloids Surf B: Biointerfaces 216:112537
Gupta M, Agrawal U, Vyas SP (2012) Nanocarrier-based topical drug delivery for the treatment of skin diseases. Expert Opin Drug Deliv 9:783–804
Hengge UR, Ruzicka T, Schwartz RA, Cork MJ (2006) Adverse effects of topical glucocorticosteroids. J Am Acad Dermatol 54:1–15
Hiraganahalli Bhaskarmurthy D, Evan Prince S (2021) Effect of Baricitinib on TPA-induced psoriasis like skin inflammation. Life Sci 279:119655
Hu L, Luo X, Zhou S, Zhu J, Xiao M, Li C, Zheng H, Qiu Q, Lai C, Liu X, Deng Y, Song Y (2019) Neutrophil-mediated delivery of dexamethasone palmitate-loaded liposomes decorated with a Sialic Acid Conjugate for Rheumatoid Arthritis Treatment. Pharm Res 36:97
Japiassu KB, Fay F, Marengo A, Mendanha SA, Cailleau C, Louaguenouni Y, Wang Q, Denis S, Tsapis N, Leite Nascimento T, Lima EM, Fattal E (2023) Hyaluronic acid-conjugated liposomes loaded with dexamethasone: a promising approach for the treatment of inflammatory diseases. Int J Pharm 639:122946
Kalaycioglu GD, Aydogan N (2016) Preparation and investigation of solid lipid nanoparticles for drug delivery. Colloids Surf a: Physicochem Eng Asp 510:77–86
Kim JK, Yuan H, Nie J, Yang YT, Leggas M, Potter PM, Rinehart J, Jay M, Lu X (2012) High payload dual therapeutic-imaging nanocarriers for triggered tumor delivery. Small 8:2895–2903
Kumar S, Randhawa JK (2013) Preparation and characterization of Paliperidone loaded solid lipid nanoparticles. Colloids Surf B: Biointerfaces 102:562–568
Lee G-Y, Zeb A, Kim E-H, Suh B, Shin Y-J, Kim D, Kim K-W, Choe Y-H, Choi H-I, Lee C-H, Qureshi OS, Han I-B, Chang S-Y, Bae O-N, Kim J-K (2020a) CORM-2-entrapped ultradeformable liposomes ameliorate acute skin inflammation in an ear edema model via effective CO delivery. Acta Pharm Sin B 10:2362–2373
Lee H, Jeong SW, Jung E, Lee D (2020b) Dexamethasone-loaded H2O2-activatable anti-inflammatory nanoparticles for on-demand therapy of inflammatory respiratory diseases. Nanomedicine 30:102301
Lee JH, Yeo Y (2015) Controlled drug release from pharmaceutical nanocarriers. Chem Eng Sci 125:75–84
Li J, Yang J, Wang W, Yu J, Fu J, Wang X (2009) A novel liposomal dexamethasone palmitate formulation and anti-inflammatory effects on mice. Chin J Chem 27:1411–1414
Liu J, Huang H, Huang Z, Ma Y, Zhang L, He Y, Li D, Liu W, Goodin S, Zhang K, Zheng X (2019) Eriocitrin in combination with resveratrol ameliorates LPS-induced inflammation in RAW264.7 cells and relieves TPA-induced mouse ear edema. J Funct Foods 56:321–332
Lopes R, Eleutério CV, Gonçalves LM, Cruz ME, Almeida AJ (2012) Lipid nanoparticles containing oryzalin for the treatment of leishmaniasis. Eur J Pharm Sci 45:442–450
Lorscheider M, Tsapis N, Simón-Vázquez R, Guiblin N, Ghermani N, Reynaud F, Canioni R, Abreu S, Chaminade P, Fattal E (2019a) Nanoscale Lipophilic Prodrugs of Dexamethasone with enhanced pharmacokinetics. Mol Pharm 16:2999–3010
Lorscheider M, Tsapis N, ur-Rehman M, Gaudin F, Stolfa I, Abreu S, Mura S, Chaminade P, Espeli M, Fattal E (2019b) Dexamethasone palmitate nanoparticles: an efficient treatment for rheumatoid arthritis. J Control Release 296:179–189
Madamsetty VS, Mohammadinejad R, Uzieliene I, Nabavi N, Dehshahri A, García-Couce J, Tavakol S, Moghassemi S, Dadashzadeh A, Makvandi P, Pardakhty A, Aghaei Afshar A, Seyfoddin A (2022) Dexamethasone: insights into pharmacological aspects, therapeutic mechanisms, and Delivery systems. ACS Biomater Sci Eng 8:1763–1790
Mandawgade SD, Patravale VB (2008) Development of SLNs from natural lipids: application to topical delivery of tretinoin. Int J Pharm 363:132–138
McDonough AK, Curtis JR, Saag KG (2008) The epidemiology of glucocorticoid-associated adverse events. Curr Opin Rheumatol 20:131–137
Müller RH, Mäder K, Gohla S (2000) Solid lipid nanoparticles (SLN) for controlled drug delivery– a review of the state of the art. Eur J Pharm Biopharm 50:161–177
Müller RH, Radtke M, Wissing SA (2002) Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) in cosmetic and dermatological preparations. Adv Drug Deliv Rev 54:S131–S155
Mohtar N, N AKK, Darwis Y (2015) Solid lipid nanoparticles of Atovaquone based on 2(4) full-Factorial Design. Iran J Pharm Res 14:989–1000
Nicolaides NC, Galata Z, Kino T, Chrousos GP, Charmandari E (2010) The human glucocorticoid receptor: molecular basis of biologic function. Steroids 75:1–12
Noreen S, Maqbool I, Madni A (2021) Dexamethasone: therapeutic potential, risks, and future projection during COVID-19 pandemic. Eur J Pharmacol 894:173854
Patil RH, Naveen Kumar M, Kiran Kumar KM, Nagesh R, Kavya K, Babu RL, Ramesh GT, Chidananda Sharma S (2018) Dexamethasone inhibits inflammatory response via down regulation of AP-1 transcription factor in human lung epithelial cells. Gene 645:85–94
Qureshi OS, Kim HS, Zeb A, Choi JS, Kim HS, Kwon JE, Kim MS, Kang JH, Ryou C, Park JS, Kim JK (2017) Sustained release docetaxel-incorporated lipid nanoparticles with improved pharmacokinetics for oral and parenteral administration. J Microencapsul 34:250–261
Qureshi OS, Zeb A, Akram M, Kim M-S, Kang J-H, Kim H-S, Majid A, Han I, Chang S-Y, Bae O-N, Kim J-K (2016) Enhanced acute anti-inflammatory effects of CORM-2-loaded nanoparticles via sustained carbon monoxide delivery. Eur J Pharm Biopharm 108:187–195
Rana I, Khan N, Ansari MM, Shah FA, Din FU, Sarwar S, Imran M, Qureshi OS, Choi HI, Lee CH, Kim JK, Zeb A (2020) Solid lipid nanoparticles-mediated enhanced antidepressant activity of duloxetine in lipopolysaccharide-induced depressive model. Colloids Surf B: Biointerfaces 194:111209
Rauchhaus U, Schwaiger FW, Panzner S (2009) Separating therapeutic efficacy from glucocorticoid side-effects in rodent arthritis using novel, liposomal delivery of dexamethasone phosphate: long-term suppression of arthritis facilitates interval treatment. Arthritis Res Ther 11:R190
Rizvi SZH, Shah FA, Khan N, Muhammad I, Ali KH, Ansari MM, Din Fu, Qureshi OS, Kim K-W, Choe Y-H, Kim J-K, Zeb A (2019) Simvastatin-loaded solid lipid nanoparticles for enhanced anti-hyperlipidemic activity in hyperlipidemia animal model. Int J Pharm 560:136–143
Rubab S, Naeem K, Rana I, Khan N, Afridi M, Ullah I, Shah FA, Sarwar S, Din Fu, Choi H-I, Lee C-H, Lim C-W, Alamro AA, Kim J-K, Zeb A (2021) Enhanced neuroprotective and antidepressant activity of curcumin-loaded nanostructured lipid carriers in lipopolysaccharide-induced depression and anxiety rat model. Int J Pharm 603:120670
Salvioni L, Morelli L, Ochoa E, Labra M, Fiandra L, Palugan L, Prosperi D, Colombo M (2021) The emerging role of nanotechnology in skincare. Adv Colloid Interface Sci 293:102437
Sara K, Mehdi A, Fateme Z, Mohsen S, Samira Sadat A, Ali Mohammad T (2022) Surface engineered palmitoyl-mesoporous silica nanoparticles with supported lipid bilayer coatings for high-capacity loading and prolonged release of dexamethasone: a factorial design approach. J Drug Deliv Sci Technol 78:103943
Shi L, Li Z, Yu L, Jia H, Zheng L (2011) Effects of surfactants and lipids on the Preparation of solid lipid nanoparticles using double Emulsion Method. J Dispers Sci Technol 32:254–259
Simón-Vázquez R, Tsapis N, Lorscheider M, Rodríguez A, Calleja P, Mousnier L, de Miguel Villegas E, González-Fernández Á, Fattal E (2022) Improving dexamethasone drug loading and efficacy in treating arthritis through a lipophilic prodrug entrapped into PLGA-PEG nanoparticles. Drug Deliv Transl Res 12:1270–1284
Son G-H, Lee B-J, Cho C-W (2017) Mechanisms of drug release from advanced drug formulations such as polymeric-based drug-delivery systems and lipid nanoparticles. J Pharm Investig 47:287–296
Souto EB, Baldim I, Oliveira WP, Rao R, Yadav N, Gama FM, Mahant S (2020) SLN and NLC for topical, dermal, and transdermal drug delivery. Expert Opin Drug Deliv 17:357–377
Wissing SA, Müller RH (2003) Cosmetic applications for solid lipid nanoparticles (SLN). Int J Pharm 254:65–68
Wolff K, Robinson K, Suh N, Michniak-Kohn B, Goedken M, Polunas M, Raskin I (2023) Isothiocyanate-rich moringa seed extract reduces skin inflammation in mouse ear edema model. Phytomed Plus 3:100479
Xu W, Lim SJ, Lee MK (2013) Cellular uptake and antitumour activity of paclitaxel incorporated into trilaurin-based solid lipid nanoparticles in ovarian cancer. J Microencapsul 30:755–761
Yasir M, Sara UVS (2014) Solid lipid nanoparticles for nose to brain delivery of haloperidol: in vitro drug release and pharmacokinetics evaluation. Acta Pharm Sin B 4:454–463
Zeb A, Arif ST, Malik M, Shah FA, Din FU, Qureshi OS, Lee E-S, Lee G-Y, Kim J-K (2019) Potential of nanoparticulate carriers for improved drug delivery via skin. J Pharm Investig 49:485–517
Zeb A, Qureshi OS, Kim HS, Kim MS, Kang JH, Park JS, Kim JK (2017) High payload itraconazole-incorporated lipid nanoparticles with modulated release property for oral and parenteral administration. J Pharm Pharmacol 69:955–966
Zeng WJ, Tan Z, Lai XF, Xu YN, Mai CL, Zhang J, Lin ZJ, Liu XG, Sun SL, Zhou LJ (2018) Topical delivery of l-theanine ameliorates TPA-induced acute skin inflammation via downregulating endothelial PECAM-1 and neutrophil infiltration and activation. Chem Biol Interact 284:69–79
Zhang J, Fan Y, Smith E (2009) Experimental design for the optimization of lipid nanoparticles. J Pharm Sci 98:1813–1819