In the transdermal drug delivery system, the drug is administered through the skin and attains a systemic effect. It is a drug administration route that includes drug transport to the epidermis and potentially dermal tissue of the skin for locally therapeutic effect, while an exceptionally significant drug division is transported in systemic blood circulation. This study aimed to formulate rasagiline mesylate (RM) as a transdermal microneedle (MN) delivery. The RM is an antiparkinson drug that can be classified as class III with low permeability and subjected to extensive first-pass metabolism. At first, it was formulated as nanoparticles using the chitosan polymer and ion gelation method. Afterward, the prepared nanoparticles were incorporated into a transdermal MN formulated by a polydimethylsiloxane template. The two-step casting process uses two polymer concentrations of polyvinyl alcohol and mixes them with other polymers in a 3:1 ratio (polyvinylpyrrolidone and chitosan) and glycerin as a plasticizer. The selected MN formula was MN4 with a promising shape, no bubbles, fine and well-formed sharp needles that passed the folding endurance test with 130 folding times before broken, drug content of 97±10.02%, and ex vivo permeation. The results showed a significant (P>0.05) permeability enhancement and increase of flux (160%), compared to the transdermal patch. The RS polymeric nanoparticles were successfully prepared and loaded within dissolving MNs of sufficient mechanical strength to penetrate the stratum corneum and enhance the amount permeated through it to induce the systemic effect transdermally. |
- Divya A, Rao M, Gnanprakash K, Sowjanya A, Vidyasagar N, Gobinath M. A review on current scenario of transdermal drug delivery system. Int J Res Pharm Sci. 2012;3(4):494-502.
- Noreen S, Pervaiz F, Ashames A, Buabeid M, Fahelelbom K, Shoukat H, et al. Optimization of novel naproxen-loaded chitosan/carrageenan nanocarrier-based gel for topical delivery: ex vivo, histopathological, and in vivo evaluation. Pharmaceuticals. 2021;14(6):557.
- Yadav MK, Pandey M, Lodhi K. Transdermal Drug Delivery Patches: Overview of Systemic Review. Int J Pharm Life sci. 2022;13(2).
- Dhiman S, Singh TG, Rehni AK. Transdermal patches: a recent approach to new drug delivery system. Int J Pharm Pharm Sci. 2011;3(5):26-34.
- Kumar L, Utreja P. Transcending the Cutaneous Barrier Through Nanocarrier Exploration for Passive Delivery of Anti-hypertensive Drugs: A Critical Review. Recent Pat Nanotechnol. 2020;14(3):193-209.
- Pereira R, Silva SG, Pinheiro M, Reis S, Vale MLd. Current status of amino acid-based permeation enhancers in transdermal drug delivery. Membranes. 2021;11(5):343.
- Préat V, Vanbever R. Skin electroporation for transdermal and topical drug delivery. Trans Drug Deliv. 2002;123:227-54.
- Thakkar HP, Savsani H, Srivastava P. Influence of Inclusion Complexation and Skin Microporation on Enhancement of Transdermal Permeation of Raloxifene Hydrochloride. Indian J Pharm Sci. 2019;81(1):22-31.
- Finberg JP, Rabey JM. Inhibitors of MAO-A and MAO-B in psychiatry and neurology. Front Pharmacol. 2016;7:340.
- Mueller BK, Schmidt M, Barlow E, Leddy M, Hsieh C-M, Bardwell P. Antibodies against the RGM A protein and uses thereof. Google Patents; 2015.
- Szökő É, Tábi T, Riederer P, Vécsei L, Magyar K. Pharmacological aspects of the neuroprotective effects of irreversible MAO-B inhibitors, selegiline and rasagiline, in Parkinson’s disease. J Neural Transm. 2018;125(11):1735-49.
- Saeed RM, Abdullah M, Ahram M, Taha MO. Novel Ellipsoid Chitosan-Phthalate Lecithin Nanoparticles for siRNA Delivery. Front Bioeng Biotechnol. 2021;9:589.
- Dong Z, Iqbal S, Zhao Z. Preparation of ergosterol-loaded nanostructured lipid carriers for enhancing oral bioavailability and antidiabetic nephropathy effects. AAPS Pharm Sci Tech. 2020;21(2):1-11.
- Alkhiro AR, Ghareeb MM. Formulation and Evaluation of Iornoxicam as Dissolving Microneedle Patch. Iraqi J Pharm Sci. 2020;29(1):184-94.
- Chen M-C, Ling M-H, Lai K-Y, Pramudityo E. Chitosan microneedle patches for sustained transdermal delivery of macromolecules. Biomacromolecules. 2012;13(12):4022-31.
- Zaman M, Hassan R, Razzaq S, Mahmood A, Amjad MW, Raja MAG, et al. Fabrication of polyvinyl alcohol based fast dissolving oral strips of sumatriptan succinate and metoclopramide HCL. Sci Prog. 2020;103(4):0036850420964302.
17. Imtiaz MS, Shoaib MH, Yousuf RI, Ali FR, Saleem MT, Khan MZ, et al. Formulation development and evaluation of drug-in-adhesive-type transdermal patch of metoclopramide HCl. Polym Bull. 2022;79(2):1187-200.
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