RSS-Feed abonnieren
Bitte kopieren Sie die angezeigte URL und fügen sie dann in Ihren RSS-Reader ein.
https://www.thieme-connect.de/rss/thieme/de/10.1055-s-00043364.xml
PDF herunterladen
CC BY 4.0 · Pharmaceutical Fronts 2024; 06(04): e439-e448
DOI: 10.1055/s-0044-1791832
DOI: 10.1055/s-0044-1791832
Original Article
Resveratrol-Loaded Dissolving Microneedles: Fabrication and in vitro Evaluation
Authors
Funding This research was funded by the Natural Science Foundation of Jiangxi Province (Grant No. 20242BAB23090), the Jiangxi University of Chinese Medicine Science and Technology Innovation Team Development Program (Grant Nos. CXTD-22008, CXTD-22004), the PhD startup foundation of Affiliated Hospital of Jiangxi University of Chinese Medicine (Grant No. 23KYQDZJ02) and the students' innovation and entrepreneurship training program (Grant Nos. 202110412009, 202210412312).
Abstract
Resveratrol (Res), an active ingredient derived from a multitude of plants, exhibits multiple pharmacological activities. However, its poor water solubility and low bioavailability present significant challenges to its clinical application. Our study aimed to improve the transdermal absorption of Res using dissolving microneedle (MN) technology, which could effectively overcome the stratum corneum barrier. Res-loaded dissolving microneedles (Res-MNs) were fabricated using polyvinyl pyrrolidone K90 (PVP K90) as the matrix material, and a two-step casting procedure was employed. The process was optimized using the Box–Behnken experimental design approach. The characteristics of Res-MNs in vitro, including morphology, solubility, safety evaluation, and skin permeation, were studied. The results showed that the optimum preparation conditions of Res-MNs were a centrifugation time of 10 minutes, a solvent concentration of 25%, and a prescription ratio (Res: matrix) of 0.375. The skin permeability of the Res-MNs was enhanced compared with Res suspension and Res gel. The cumulative release of Res-MNs in vitro was 75%, which was approximately 5 and 3 times that of the Res suspension group and Res gel group. These results suggest that dissolving MNs may represent a potential approach for enhancing the transdermal delivery of poorly absorbed drugs such as Res.
Ethical Approval
This work was approved by the Animal Ethics Committee and abides by the relevant agreements of the National Pharmaceutical Engineering Center for Solid Preparation in Chinese Herbal Medicine, Jiangxi University of Traditional Chinese Medicine.
Publikationsverlauf
Eingereicht: 22. November 2023
Angenommen: 24. September 2024
Artikel online veröffentlicht:
08. November 2024
© 2024. The Author(s). This is an open access article published by Thieme under the terms of the Creative Commons Attribution License, permitting unrestricted use, distribution, and reproduction so long as the original work is properly cited. (https://creativecommons.org/licenses/by/4.0/)
Georg Thieme Verlag KG
Rüdigerstraße 14, 70469 Stuttgart, Germany
-
References
- 1 Ren J, Liu H, Hao Y, He P, Fang Y. Determination of resveratrol in red wine by solid phase extraction-flow injection chemiluminescence method. Chin Chem Lett 2007; 18: 985-988
- 2 Zhang Q, Bian Y, Shi Y. et al. An economical and efficient technology for the extraction of resveratrol from peanut (Arachis hypogaea) sprouts by multi-stage countercurrent extraction. Food Chem 2015; 179: 15-25
- 3 Ros E, Singh A, O'Keefe JH. Nuts: natural pleiotropic nutraceuticals. Nutrients 2021; 13 (09) 3269
- 4 Abdel Bar FM, Abbas GM, Gohar AA, Lahloub MI. Antiproliferative activity of stilbene derivatives and other constituents from the stem bark of Morus nigra L. Nat Prod Res 2020; 34 (24) 3506-3513
- 5 Ungurianu A, Zanfirescu A, Margină D. Sirtuins, resveratrol and the intertwining cellular pathways connecting them. Ageing Res Rev 2023; 88: 101936
- 6 Chedea VS, Vicaş SI, Sticozzi C. et al. Resveratrol: from diet to topical usage. Food Funct 2017; 8 (11) 3879-3892
- 7 Cho S, Namkoong K, Shin M. et al. Cardiovascular protective effects and clinical applications of resveratrol. J Med Food 2017; 20 (04) 323-334
- 8 Ko JH, Sethi G, Um JY. et al. The role of resveratrol in cancer therapy. Int J Mol Sci 2017; 18 (12) 2589
- 9 Kotecha R, Takami A, Espinoza JL. Dietary phytochemicals and cancer chemoprevention: a review of the clinical evidence. Oncotarget 2016; 7 (32) 52517-52529
- 10 Nawaz W, Zhou Z, Deng S. et al. Therapeutic versatility of resveratrol derivatives. Nutrients 2017; 9 (11) 1188
- 11 Tang H, Xiang S, Li X, Zhou J, Kuang C. Preparation and in vitro performance evaluation of resveratrol for oral self-microemulsion. PLoS One 2019; 14 (04) e0214544
- 12 Annaji M, Poudel I, Boddu SHS, Arnold RD, Tiwari AK, Babu RJ. Resveratrol-loaded nanomedicines for cancer applications. Cancer Rep (Hoboken) 2021; 4 (03) e1353
- 13 Tosato MG, Maya Girón JV, Martin AA, Krishna Tippavajhala V, Fernández Lorenzo de Mele M, Dicelio L. Comparative study of transdermal drug delivery systems of resveratrol: high efficiency of deformable liposomes. Mater Sci Eng C 2018; 90: 356-364
- 14 Sinha D, Sarkar N, Biswas J, Bishayee A. Resveratrol for breast cancer prevention and therapy: preclinical evidence and molecular mechanisms. Semin Cancer Biol 2016; 40-41: 209-232
- 15 Pujara N, Jambhrunkar S, Wong KY, McGuckin M, Popat A. Enhanced colloidal stability, solubility and rapid dissolution of resveratrol by nanocomplexation with soy protein isolate. J Colloid Interface Sci 2017; 488: 303-308
- 16 Qu F, Geng R, Liu Y, Zhu J. Advanced nanocarrier- and microneedle-based transdermal drug delivery strategies for skin diseases treatment. Theranostics 2022; 12 (07) 3372-3406
- 17 Zhang Y, Liu C, Wang JQ. et al. Ionic liquids in transdermal drug delivery system: current applications and future perspectives. Chin Chem Lett 2023; 34: 107631
- 18 Alany R. Topical and transdermal formulation and drug delivery. Pharm Dev Technol 2017; 22 (04) 457
- 19 Prausnitz MR, Langer R. Transdermal drug delivery. Nat Biotechnol 2008; 26 (11) 1261-1268
- 20 Dharadhar S, Majumdar A, Dhoble S, Patravale V. Microneedles for transdermal drug delivery: a systematic review. Drug Dev Ind Pharm 2019; 45 (02) 188-201
- 21 Zhang X, Wang Y, Chi J, Zhao Y. Smart microneedles for therapy and diagnosis. Research (Wash D C) 2020; 2020: 7462915
- 22 Zuo J, Du L, Li M, Liu B, Zhu W, Jin Y. Transdermal enhancement effect and mechanism of iontophoresis for non-steroidal anti-inflammatory drugs. Int J Pharm 2014; 466 (1-2): 76-82
- 23 Andrade JFM, Cunha-Filho M, Gelfuso GM, Gratieri T. Iontophoresis for the cutaneous delivery of nanoentraped drugs. Expert Opin Drug Deliv 2023; 20 (06) 785-798
- 24 Seah BC, Teo BM. Recent advances in ultrasound-based transdermal drug delivery. Int J Nanomedicine 2018; 13: 7749-7763
- 25 Sammeta SM, Repka MA, Narasimha Murthy S. Magnetophoresis in combination with chemical enhancers for transdermal drug delivery. Drug Dev Ind Pharm 2011; 37 (09) 1076-1082
- 26 Huang D, Huang Y, Li Z. Transdermal delivery of nucleic acid-mediated by punching and electroporation. Methods Mol Biol 2020; 2050: 101-112
- 27 Zhang H, Jin WR. Determination of amino acids in an individual erythrocyteby capillary electrophoresis with intracellular FITC-derivatization and laser-induced fluorescence detection. Chin Chem Lett 2003; 14: 952-954
- 28 Dradrach K, Rogóż M, Grabowski P. et al. Traveling wave rotary micromotor based on a photomechanical response in liquid crystal polymer networks. ACS Appl Mater Interfaces 2020; 12 (07) 8681-8686
- 29 Sharma D. Microneedles: an approach in transdermal drug delivery: a review. Pharmatutor 2018; 6: 07
- 30 Ali MK, Moshikur RM, Goto M, Moniruzzaman M. Recent developments in ionic liquid-assisted topical and transdermal drug delivery. Pharm Res 2022; 39 (10) 2335-2351
- 31 Park D, Won J, Lee G, Lee Y, Kim CW, Seo J. Sonophoresis with ultrasound-responsive liquid-core nuclei for transdermal drug delivery. Skin Res Technol 2022; 28 (02) 291-298
- 32 Chen Z, Lv Y, Qi J, Zhu Q, Lu Y, Wu W. Overcoming or circumventing the stratum corneum barrier for efficient transcutaneous immunization. Drug Discov Today 2018; 23 (01) 181-186
- 33 Pireddu R, Schlich M, Marceddu S. et al. Nanosuspensions and microneedles roller as a combined approach to enhance diclofenac topical bioavailability. Pharmaceutics 2020; 12 (12) 1140
- 34 Sheng T, Luo B, Zhang W. et al. Microneedle-mediated vaccination: innovation and translation. Adv Drug Deliv Rev 2021; 179: 113919
- 35 Ramaut L, Hoeksema H, Pirayesh A, Stillaert F, Monstrey S. Microneedling: where do we stand now? A systematic review of the literature. J Plast Reconstr Aesthet Surg 2018; 71 (01) 1-14
- 36 Kapoor Y, Milewski M, Dick L. et al. Coated microneedles for transdermal delivery of a potent pharmaceutical peptide. Biomed Microdevices 2019; 22 (01) 7
- 37 Chen Z, He J, Qi J, Zhu Q, Wu W, Lu Y. Long-acting microneedles: a progress report of the state-of-the-art techniques. Drug Discov Today 2020; 25 (08) 1462-1468
- 38 Tan JY, Li Y, Chamani F. et al. Experimental validation of diffraction lithography for fabrication of solid microneedles. Materials (Basel) 2022; 15 (24) 8934
- 39 Cárcamo-Martínez Á, Mallon B, Domínguez-Robles J, Vora LK, Anjani QK, Donnelly RF. Hollow microneedles: a perspective in biomedical applications. Int J Pharm 2021; 599: 120455
- 40 Matadh AV, Jakka D, Pragathi SG. et al. Polymer-coated polymeric (PCP) microneedles for controlled dermal delivery of 5-fluorouracil. AAPS PharmSciTech 2022; 24 (01) 9
- 41 Sartawi Z, Blackshields C, Faisal W. Dissolving microneedles: applications and growing therapeutic potential. J Control Release 2022; 348: 186-205
- 42 Liu Y, Huang T, Qian ZY, Chen W. Extensible and swellable hydrogel-forming microneedles for deep point-of-care sampling and drug deployment. Chin Chem Lett 2023; 34: 108103
- 43 Ita K. Dissolving microneedles for transdermal drug delivery: advances and challenges. Biomed Pharmacother 2017; 93: 1116-1127
- 44 Sullivan SP, Koutsonanos DG, Del Pilar Martin M. et al. Dissolving polymer microneedle patches for influenza vaccination. Nat Med 2010; 16 (08) 915-920
- 45 Ronnander P, Simon L, Koch A. Experimental and mathematical study of the transdermal delivery of sumatriptan succinate from polyvinylpyrrolidone-based microneedles. Eur J Pharm Biopharm 2020; 146: 32-40
- 46 Song YY, Dong CM. Sugar-dependent targeting and immune adjuvant effects of hyperbranched glycosylated polypeptide nanoparticles for ovalbumin delivery. Chin Chem Lett 2022; 33: 4084-4088
- 47 Nguyen HX, Bozorg BD, Kim Y. et al. Poly (vinyl alcohol) microneedles: fabrication, characterization, and application for transdermal drug delivery of doxorubicin. Eur J Pharm Biopharm 2018; 129: 88-103
- 48 Wu L, Shrestha P, Iapichino M, Cai Y, Kim B, Stoeber B. Characterization method for calculating diffusion coefficient of drug from polylactic acid (PLA) microneedles into the skin. J Drug Deliv Transl 2021; 61: 102192
- 49 He J, Zhang Z, Zheng X. et al. Design and evaluation of dissolving microneedles for enhanced dermal delivery of propranolol hydrochloride. Pharmaceutics 2021; 13 (04) 579
- 50 Maurya A, Nanjappa SH, Honnavar S, Salwa M, Murthy SN. Rapidly dissolving microneedle patches for transdermal iron replenishment therapy. J Pharm Sci 2018; 107 (06) 1642-1647
- 51 Pei P, Yang F, Liu J. et al. Composite-dissolving microneedle patches for chemotherapy and photothermal therapy in superficial tumor treatment. Biomater Sci 2018; 6 (06) 1414-1423
- 52 Ahmed Saeed Al-Japairai K, Mahmood S, Hamed Almurisi S. et al. Current trends in polymer microneedle for transdermal drug delivery. Int J Pharm 2020; 587: 119673
- 53 Hong X, Wei L, Wu F. et al. Dissolving and biodegradable microneedle technologies for transdermal sustained delivery of drug and vaccine. Drug Des Devel Ther 2013; 7: 945-952
- 54 Zhang L, Dong Z, Liu W. et al. Novel Pharmaceutical strategies for enhancing skin penetration of biomacromolecules. Pharmaceuticals (Basel) 2022; 15 (07) 877
- 55 Chen YH, Lin DC, Chern E, Huang YY. The use of micro-needle arrays to deliver cells for cellular therapies. Biomed Microdevices 2020; 22 (04) 63
- 56 Yang H, Kang G, Jang M. et al. Development of lidocaine-loaded dissolving microneedle for rapid and efficient local anesthesia. Pharmaceutics 2020; 12 (11) 1067
- 57 Yu Q, Huang Y, Zhu C. et al. Combination of microneedles and MF59 adjuvant as a simple approach to enhance transcutaneous immunization. J Biomed Nanotechnol 2020; 16 (12) 1776-1786
- 58 Dalvi M, Kharat P, Thakor P, Bhavana V, Singh SB, Mehra NK. Panorama of dissolving microneedles for transdermal drug delivery. Life Sci 2021; 284: 119877
- 59 Cheng M, Yuan F, Liu J. et al. Fabrication of fine puerarin nanocrystals by Box-Behnken design to enhance intestinal absorption. AAPS PharmSciTech 2020; 21 (03) 90
- 60 Rouphael NG, Paine M, Mosley R. et al; TIV-MNP 2015 Study Group. The safety, immunogenicity, and acceptability of inactivated influenza vaccine delivered by microneedle patch (TIV-MNP 2015): a randomised, partly blinded, placebo-controlled, phase 1 trial. Lancet 2017; 390 (10095): 649-658
- 61 Van Damme P, Oosterhuis-Kafeja F, Van der Wielen M, Almagor Y, Sharon O, Levin Y. Safety and efficacy of a novel microneedle device for dose sparing intradermal influenza vaccination in healthy adults. Vaccine 2009; 27 (03) 454-459
- 62 Chatterjee B, Reddy A, Santra M, Khamanga S. Amorphization of drugs for transdermal delivery-a recent update. Pharmaceutics 2022; 14 (05) 983
- 63 Yoon DS, Choi Y, Jang Y. et al. SIRT1 directly regulates SOX2 to maintain self-renewal and multipotency in bone marrow-derived mesenchymal stem cells. Stem Cells 2014; 32 (12) 3219-3231
- 64 Qiang N, Liu Z, Lu M. et al. Preparation and properties of polyvinylpyrrolidone/sodium carboxymethyl cellulose soluble microneedles. Materials (Basel) 2023; 16 (09) 3417
- 65 Aung NN, Ngawhirunpat T, Rojanarata T, Patrojanasophon P, Opanasopit P, Pamornpathomkul B. HPMC/PVP dissolving microneedles: a promising delivery platform to promote trans-epidermal delivery of alpha-arbutin for skin lightening. AAPS PharmSciTech 2019; 21 (01) 25
- 66 Wang Q, Yao G, Dong P. et al. Investigation on fabrication process of dissolving microneedle arrays to improve effective needle drug distribution. Eur J Pharm Sci 2015; 66: 148-156
- 67 Al-Saidan SM, Krishnaiah YS, Chandrasekhar DV. et al. Formulation of an HPMC gel drug reservoir system with ethanol-water as a solvent system and limonene as a penetration enhancer for enhancing in vitro transdermal delivery of nicorandil. Skin Pharmacol Physiol 2004; 17 (06) 310-320
- 68 Kovačević M, Zvonar Pobirk A, German Ilić I. The effect of polymeric binder type and concentration on flow and dissolution properties of SMEDDS loaded mesoporous silica-based granules. Eur J Pharm Sci 2024; 193: 106582
- 69 Du H, Liu P, Zhu J. et al. Hyaluronic acid-based dissolving microneedle patch loaded with methotrexate for improved treatment of psoriasis. ACS Appl Mater Interfaces 2019; 11 (46) 43588-43598
- 70 Waghule T, Singhvi G, Dubey SK. et al. Microneedles: a smart approach and increasing potential for transdermal drug delivery system. Biomed Pharmacother 2019; 109: 1249-1258
- 71 Bala P, Jathar S, Kale S. et al. Transdermal drug delivery system (TDDS)-a multifaceted approach for drug delivery. J Pharm Res 2014; 8 (12) 1805-1835