Development and Optimization of Imiquimod-Loaded Nanostructured Lipid Carriers Using a Hybrid Design of Experiments Approach

References

• Hanna E, Abadi R, Abbas O. Imiquimod in dermatology: an overview. Int J Dermatol. 2016;55(8):831–844. doi:10.1111/ijd.13235
   PubMed Web of Science ®Google Scholar
• Ghezzi M, Pescina S, Delledonne A, et al. Improvement of imiquimod solubilization and skin retention via TPGS micelles: exploiting the co-solubilizing effect of oleic acid. Pharmaceutics. 2021;13(9):1476. doi:10.3390/pharmaceutics13091476
   PubMed Web of Science ®Google Scholar
• Sabri AH, Cater Z, Gurnani P, et al. Intradermal delivery of imiquimod using polymeric microneedles for basal cell carcinoma. Int J Pharm. 2020;589:119808. doi:10.1016/j.ijpharm.2020.119808
   PubMedGoogle Scholar
• Lapteva M, Mignot M, Mondon K, Moller M, Gurny R, Kalia YN. Self-assembled mPEG-hexPLA polymeric nanocarriers for the targeted cutaneous delivery of imiquimod. Eur J Pharm Biopharm. 2019;142:553–562. doi:10.1016/j.ejpb.2019.01.008
   PubMed Web of Science ®Google Scholar
• Jamshaid H, Din F, Malik M, et al. A cutback in Imiquimod cutaneous toxicity; comparative cutaneous toxicity analysis of Imiquimod nanotransethosomal gel with 5% marketed cream on the BALB/c mice. Sci Rep. 2022;12(1):14244. doi:10.1038/s41598-022-18671-1
   PubMed Web of Science ®Google Scholar
• Telo I, Favero ED, Cantu L, et al. Gel-like TPGS-based microemulsions for imiquimod dermal delivery: role of mesostructure on the uptake and distribution into the skin. Mol Pharm. 2017;14(10):3281–3289. doi:10.1021/acs.molpharmaceut.7b00348
   PubMedGoogle Scholar
• Hua S. Lipid-based nano-delivery systems for skin delivery of drugs and bioactives. Front Pharmacol. 2015;6:219. doi:10.3389/fphar.2015.00219
   PubMed Web of Science ®Google Scholar
• Algahtani MS, Ahmad MZ, Nourein IH, Ahmad J. Co-delivery of imiquimod and curcumin by nanoemugel for improved topical delivery and reduced psoriasis-like skin lesions. Biomolecules. 2020;10(7):968. doi:10.3390/biom10070968
   PubMed Web of Science ®Google Scholar
• Venturini CG, Bruinsmann FA, Contri RV, et al. Co-encapsulation of imiquimod and copaiba oil in novel nanostructured systems: promising formulations against skin carcinoma. Eur J Pharm Sci. 2015;79:36–43. doi:10.1016/j.ejps.2015.08.016
   PubMed Web of Science ®Google Scholar
• Zhou HF, Ma Q-H, Xia Q, et al. Preparation and characteristics of imiquimod-loaded solid lipid nanoparticles. Chin Pharm J. 2006;41:1084–1088,1120.
   Google Scholar
• Elsewedy HS, Shehata TM, Soliman WE. Shea butter potentiates the anti-bacterial activity of fusidic acid incorporated into solid lipid nanoparticle. Polymers. 2022;14(12):2436. doi:10.3390/polym14122436
   PubMed Web of Science ®Google Scholar
• Stefanov SR, Andonova VY. Lipid nanoparticulate drug delivery systems: recent advances in the treatment of skin disorders. Pharmaceuticals. 2021;14(11):1083. doi:10.3390/ph14111083
   Web of Science ®Google Scholar
• Iqubal MK, Iqubal A, Imtiyaz K, et al. Combinatorial lipid-nanosystem for dermal delivery of 5-fluorouracil and resveratrol against skin cancer: delineation of improved dermatokinetics and epidermal drug deposition enhancement analysis. Eur J Pharm Biopharm. 2021;163:223–239. doi:10.1016/j.ejpb.2021.04.007
   PubMed Web of Science ®Google Scholar
• Haider M, Abdin SM, Kamal L, Orive G. Nanostructured lipid carriers for delivery of chemotherapeutics: a review. Pharmaceutics. 2020;12(3):288. doi:10.3390/pharmaceutics12030288
   PubMed Web of Science ®Google Scholar
• Kim S, Fouladian P, Afinjuomo F, et al. Effect of plasticizers on drug-in-adhesive patches containing 5-fluorouracil. Int J Pharm. 2022;611:121316. doi:10.1016/j.ijpharm.2021.121316
   PubMed Web of Science ®Google Scholar
• Arunprasert K, Pornpitchanarong C, Piemvuthi C, et al. Nanostructured lipid carrier-embedded polyacrylic acid transdermal patches for improved transdermal delivery of capsaicin. Eur J Pharma Sci. 2022;173:106169. doi:10.1016/j.ejps.2022.106169
   PubMed Web of Science ®Google Scholar
• Kumar R, Mittal A, Kulkarni MP. Quality by design in pharmaceutical development. In: Saharan VA, editor. Computer Aided Pharmaceutics and Drug Delivery: An Application Guide for Students and Researchers of Pharmaceutical Sciences. Singapore: Springer Nature; 2022:99–127. doi:10.1007/978-981-16-5180-9_4
   Google Scholar
• Subramaniam B, Siddik ZH, Nagoor NH. Optimization of nanostructured lipid carriers: understanding the types, designs, and parameters in the process of formulations. J Nanopart Res. 2020;22(6):141. doi:10.1007/s11051-020-04848-0
   Web of Science ®Google Scholar
• Alam T, Khan S, Gaba B, Haider MF, Baboota S, Ali J. Adaptation of quality by design-based development of isradipine nanostructured-lipid carrier and its evaluation for in vitro gut permeation and in vivo solubilization fate. J Pharm Sci. 2018;107(11):2914–2926. doi:10.1016/j.xphs.2018.07.021
   PubMed Web of Science ®Google Scholar
• Belkhir L, Elmeligi A. Carbon footprint of the global pharmaceutical industry and relative impact of its major players. J Clean Prod. 2019;214:185–194. doi:10.1016/j.jclepro.2018.11.204
   Web of Science ®Google Scholar
• Anastas PT. Origins and early history of green chemistry. In: Horváth I, editor. Advanced Green Chemistry. World Scientific; 2018:1–17. Available from: doi:10.1142/9789813228115_0001.
   Google Scholar
• Anastas P, Eghbali N. Green chemistry: principles and practice. Chem Soc Rev. 2010;39(1):301–312. doi:10.1039/B918763B
   PubMed Web of Science ®Google Scholar
• Gałuszka A, Migaszewski Z, Namieśnik J. The 12 principles of green analytical chemistry and the SIGNIFICANCE mnemonic of green analytical practices. Trends Anal Chem. 2013;50:78–84. doi:10.1016/j.trac.2013.04.010
   Web of Science ®Google Scholar
• Keith LH, Gron LU, Young JL. Green analytical methodologies. Chem Rev. 2007;107(6):2695–2708. doi:10.1021/cr068359e
   PubMed Web of Science ®Google Scholar
• Raynie D, Driver J. Green assessment of chemical methods. Presented at 13th Green Chemistry and Engineering Conference; USA; 2009.
   Google Scholar
• Gałuszka A, Migaszewski ZM, Konieczka P, Namieśnik J. Analytical eco-scale for assessing the greenness of analytical procedures. Trends Anal Chem. 2012;37:61–72. doi:10.1016/j.trac.2012.03.013
   Web of Science ®Google Scholar
• Płotka-Wasylka J, Mohamed HM, Kurowska-Susdorf A, Dewani R, Fares MY, Andruch V. Green analytical chemistry as an integral part of sustainable education development. Curr Opin Green Sustain Chem. 2021;31:100508. doi:10.1016/j.cogsc.2021.100508
   Web of Science ®Google Scholar
• Pena-Pereira F, Wojnowski W, Tobiszewski M. AGREE—Analytical GREEnness metric approach and software. Anal Chem. 2020;92(14):10076–10082. doi:10.1021/acs.analchem.0c01887
   PubMed Web of Science ®Google Scholar
• Kim S, Youssef SH, Song Y, Garg S. Development and application of a chromatographic method for simultaneous quantification of 5-fluorouracil and imiquimod in drug-in-adhesive topical patches. Sustain Chem Pharm. 2022;27:100711. doi:10.1016/j.scp.2022.100711
   Web of Science ®Google Scholar
• Gaba B, Fazil M, Khan S, Ali A, Baboota S, Ali J. Nanostructured lipid carrier system for topical delivery of terbinafine hydrochloride. Bull Fac Pharm. 2015;53(2):147–159. doi:10.1016/j.bfopcu.2015.10.001
   Google Scholar
• Singh S, Singh M, Tripathi CB, Arya M, Saraf SA. Development and evaluation of ultra-small nanostructured lipid carriers: novel topical delivery system for athlete’s foot. Drug Deliv Transl Res. 2016;6(1):38–47. doi:10.1007/s13346-015-0263-x
   PubMed Web of Science ®Google Scholar
• Imran M, Iqubal MK, Imtiyaz K, et al. Topical nanostructured lipid carrier gel of quercetin and resveratrol: formulation, optimization, in vitro and ex vivo study for the treatment of skin cancer. Int J Pharm. 2020;587:119705. doi:10.1016/j.ijpharm.2020.119705
   PubMed Web of Science ®Google Scholar
• Uppuluri CT, Ravi PR, Dalvi AV. Design, optimization and pharmacokinetic evaluation of Piribedil loaded solid lipid nanoparticles dispersed in nasal in situ gelling system for effective management of Parkinson’s disease. Int J Pharm. 2021;606:120881. doi:10.1016/j.ijpharm.2021.120881
   PubMedGoogle Scholar
• Sivadasan D, Sultan MH, Madkhali OA, Alsabei SH, Alessa AA. Stealth liposomes (PEGylated) containing an anticancer drug camptothecin: in vitro characterization and in vivo pharmacokinetic and tissue distribution study. Molecules. 2022;27(3):1086. doi:10.3390/molecules27031086
   PubMed Web of Science ®Google Scholar
• Vlaia L, Olariu I, Muţ AM, et al. New, biocompatible, chitosan-gelled microemulsions based on essential oils and sucrose esters as nanocarriers for topical delivery of fluconazole. Pharmaceutics. 2022;14(1):75. doi:10.3390/pharmaceutics14010075
   Web of Science ®Google Scholar
• Al-Mayahy MH, Sabri AH, Rutland CS, et al. Insight into imiquimod skin permeation and increased delivery using microneedle pre-treatment. Eur J Pharm Biopharm. 2019;139:33–43. doi:10.1016/j.ejpb.2019.02.006
   PubMed Web of Science ®Google Scholar
• Sabri A, Ogilvie J, McKenna J, Segal J, Scurr D, Marlow M. Intradermal delivery of an immunomodulator for basal cell carcinoma; expanding the mechanistic insight into solid microneedle-enhanced delivery of hydrophobic molecules. Mol Pharm. 2020;17(8):2925–2937. doi:10.1021/acs.molpharmaceut.0c00347
   PubMedGoogle Scholar
• Kaithwas V, Dora CP, Kushwah V, Jain S. Nanostructured lipid carriers of olmesartan medoxomil with enhanced oral bioavailability. Colloids Surf B Biointerfaces. 2017;154:10–20. doi:10.1016/j.colsurfb.2017.03.006
   PubMed Web of Science ®Google Scholar
• Mukherjee S, Ray S, Thakur RS. Solid lipid nanoparticles: a modern formulation approach in drug delivery system. Indian J Pharm Sci. 2009;71(4):349–358. doi:10.4103/0250-474x.57282
   PubMed Web of Science ®Google Scholar
• Telo I, Pescina S, Padula C, Santi P, Nicoli S. Mechanisms of imiquimod skin penetration. Int J Pharm. 2016;511(1):516–523. doi:10.1016/j.ijpharm.2016.07.043
   PubMedGoogle Scholar
• Rathod VR, Shah DA, Dave RH. Systematic implementation of quality-by-design (QbD) to develop NSAID-loaded nanostructured lipid carriers for ocular application: preformulation screening studies and statistical hybrid-design for optimization of variables. Drug Dev Ind Pharm. 2020;46(3):443–455. doi:10.1080/03639045.2020.1724135
   PubMed Web of Science ®Google Scholar
• Mahant S, Rao R, Souto EB, Nanda S. Analytical tools and evaluation strategies for nanostructured lipid carrier-based topical delivery systems. Expert Opin Drug Deliv. 2020;17(7):963–992. doi:10.1080/17425247.2020.1772750
   PubMed Web of Science ®Google Scholar
• Pandey SS, Patel MA, Desai DT, et al. Bioavailability enhancement of repaglinide from transdermally applied nanostructured lipid carrier gel: optimization, in vitro and in vivo studies. J Drug Deliv Sci Technol. 2020;57:101731. doi:10.1016/j.jddst.2020.101731
   Web of Science ®Google Scholar
• Baig MS, Owida H, Njoroge W, Siddiqui AR, Yang Y. Development and evaluation of cationic nanostructured lipid carriers for ophthalmic drug delivery of besifloxacin. J Drug Deliv Sci Technol. 2020;55:101496. doi:10.1016/j.jddst.2019.101496
   Web of Science ®Google Scholar
• Badawi N, El-Say K, Attia D, El-Nabarawi M, Elmazar M, Teaima M. Development of pomegranate extract-loaded solid lipid nanoparticles: quality by design approach to screen the variables affecting the quality attributes and characterization. ACS Omega. 2020;5(34):21712–21721. doi:10.1021/acsomega.0c02618
   PubMed Web of Science ®Google Scholar
• Yokota J, Kyotani S. Influence of nanoparticle size on the skin penetration, skin retention and anti-inflammatory activity of non-steroidal anti-inflammatory drugs. J Chin Med Assoc. 2018;81(6):511–519. doi:10.1016/j.jcma.2018.01.008
   PubMed Web of Science ®Google Scholar
• Jung M, Jin M, Jeon W-J, et al. Development of a long-acting tablet with ticagrelor high-loaded nanostructured lipid carriers. Drug Deliv Transl Res. 2022. doi:10.1007/s13346-022-01205-7
   Web of Science ®Google Scholar
• Witayaudom P, Klinkesorn U. Effect of surfactant concentration and solidification temperature on the characteristics and stability of nanostructured lipid carrier (NLC) prepared from rambutan (Nephelium lappaceum L.) kernel fat. J Colloid Interface Sci. 2017;505:1082–1092. doi:10.1016/j.jcis.2017.07.008
   PubMed Web of Science ®Google Scholar
• Shah B, Khunt D, Bhatt H, Misra M, Padh H. Application of quality by design approach for intranasal delivery of rivastigmine loaded solid lipid nanoparticles: effect on formulation and characterization parameters. Eur J Pharm Sci. 2015;78:54–66. doi:10.1016/j.ejps.2015.07.002
   PubMed Web of Science ®Google Scholar
• Yang Z, He Q, Ismail BB, Hu Y, Guo M. Ultrasonication induced nano-emulsification of thyme essential oil: optimization and antibacterial mechanism against Escherichia coli. Food Control. 2022;133:108609. doi:10.1016/j.foodcont.2021.108609
   Web of Science ®Google Scholar
• Rahman Z, Zidan AS, Habib MJ, Khan MA. Understanding the quality of protein loaded PLGA nanoparticles variability by Plackett–Burman design. Int J Pharm. 2010;389(1):186–194. doi:10.1016/j.ijpharm.2009.12.040
   PubMed Web of Science ®Google Scholar
• Klinkesorn U, Namatsila Y. Influence of chitosan and NaCl on physicochemical properties of low-acid tuna oil-in-water emulsions stabilized by non-ionic surfactant. Food Hydrocoll. 2009;23(5):1374–1380. doi:10.1016/j.foodhyd.2008.11.002
   Web of Science ®Google Scholar
• Remiro PR, Rosa PT, Moraes ÂM. Effect of process variables on imiquimod micronization using a supercritical antisolvent (SAS) precipitation technique. J Supercrit Fluids. 2022;181:105500. doi:10.1016/j.supflu.2021.105500
   Web of Science ®Google Scholar
• Guilherme VA, Ribeiro LNM, Alcântara ACS, et al. Improved efficacy of naproxen-loaded NLC for temporomandibular joint administration. Sci Rep. 2019;9(1):11160. doi:10.1038/s41598-019-47486-w
   PubMedGoogle Scholar
• Gupta V, Dhote V, Paul BN, Trivedi P. Development of novel topical drug delivery system containing cisplatin and imiquimod for dual therapy in cutaneous epithelial malignancy. J Liposome Res. 2014;24(2):150–162. doi:10.3109/08982104.2013.865216
   PubMed Web of Science ®Google Scholar
• Argenziano M, Haimhoffer A, Bastiancich C, et al. In vitro enhanced skin permeation and retention of imiquimod loaded in beta-cyclodextrin nanosponge hydrogel. Pharmaceutics. 2019;11(3):138. doi:10.3390/pharmaceutics11030138
   PubMed Web of Science ®Google Scholar
• Ramineni SK, Cunningham LL, Dziubla TD, Puleo DA. Development of imiquimod-loaded mucoadhesive films for oral dysplasia. J Pharm Sci. 2013;102(2):593–603. doi:10.1002/jps.23386
   PubMed Web of Science ®Google Scholar
• Gazzi RP, Frank LA, Onzi G, Pohlmann AR, Guterres SS. New pectin-based hydrogel containing imiquimod-loaded polymeric nanocapsules for melanoma treatment. Drug Deliv Transl Res. 2020;10(6):1829–1840. doi:10.1007/s13346-020-00805-5
   PubMed Web of Science ®Google Scholar
• Harrison LI, Stoesz JD, Battiste JL, Nelson RJ, Zarraga IE. A pharmaceutical comparison of different commercially available imiquimod 5% cream products. J Dermatol Treat. 2009;20(3):160–164. doi:10.1080/09546630802513693
   Web of Science ®Google Scholar
• Chollet JL, Jozwiakowski MJ, Phares KR, et al. Development of a topically active imiquimod formulation. Pharm Dev Technol. 1999;4(1):35–43. doi:10.1080/10837459908984222
   PubMed Web of Science ®Google Scholar
• Costa P, Sousa Lobo JM. Modeling and comparison of dissolution profiles. Eur J Pharm Sci. 2001;13(2):123–133. doi:10.1016/S0928-0987(01)00095-1
   PubMed Web of Science ®Google Scholar
• Hopfenberg HB. Controlled release from erodible slabs, cylinders, and spheres. In: Paul DR, Harris FW editors. Controlled Release Polymeric Formulations. American Chemical Society; 1976:26–32. doi:10.1021/bk-1976-0033.ch003
   Google Scholar
• Ruela ALM, Perissinato AG, Lino ME, Mudrik PS, Pereira GR. Evaluation of skin absorption of drugs from topical and transdermal formulations. Braz J Pharm Sci. 2016;52(3):527–544. doi:10.1590/s1984-82502016000300018
   Web of Science ®Google Scholar
• Lertpairod J, Tiyaboonchai W. pH-sensitive beads containing curcumin loaded nanostructured lipid carriers for a colon targeted oral delivery system. J Pharm Investig. 2022;52(3):387–396. doi:10.1007/s40005-022-00572-0
   Web of Science ®Google Scholar
• Abdella S, Afinjuomo F, Song Y, Upton R, Garg S. Mucoadhesive buccal film of estradiol for hormonal replacement therapy: development and in-vivo performance prediction. Pharmaceutics. 2022;14(3):542. doi:10.3390/pharmaceutics14030542
   PubMed Web of Science ®Google Scholar
• Finnin B, Walters KA, Franz TJ. In vitro skin permeation methodology. In: Benson HA, Watkinson AC editors. Topical and Transdermal Drug Delivery. John Wiley & Sons; 2011:85–108. doi:10.1002/9781118140505.ch5
   Google Scholar
• Anantaworasakul P, Chaiyana W, Michniak-Kohn BB, Rungseevijitprapa W, Ampasavate C. Enhanced transdermal delivery of concentrated capsaicin from chili extract-loaded lipid nanoparticles with reduced skin irritation. Pharmaceutics. 2020;12(5):463. doi:10.3390/pharmaceutics12050463
   PubMed Web of Science ®Google Scholar
• The United States Food and Drug Administration. Aldara (imiquimod) cream; 2010. Available from: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/020723s022lbl.pdf. Accessed January 25, 2022.
   Google Scholar