Abstract
Objective: The present investigation highlights the formulation and evaluation of nanosuspension- loaded transdermal patches of poorly soluble antilipidemic drug (rosuvastatin).
Methods: Dissolution characteristics of drug was improved by preparation of nanosuspension employing precipitation–ultrasonication technique using a different blend of water-soluble film forming polymers such as hydroxyl propyl methyl cellulose (HPMC K4M), Eudragit and were further characterized by fourier transformation infrared spectroscopy (FTIR), Malvern zetasizer and SEM. Propylene glycol and tween 80 were used as stabilizers. Based on the particle size of the formulation, the best one of NS4 was selected and fabricated into the transdermal patch by solvent casting method. The prepared formulations were evaluated for various parameters like drug excipient compatibility, appearance, morphology, thickness, tensile strength, folding endurance, % elongation, % moisture content, % moisture uptake, % drug content, in-vitro drug permeation, and stability studies were performed for the optimized formula according to the ICH Q1A (R2) guideline under 4°C and 25°C RH for three months.
Results: Amongst all formulation, P4 transdermal patches were considered the optimized formulation. It has the highest in-vitro drug permeation (86.01±0.05%), thickness (0.86±0.09), weight uniformity (475.0±8.60 mg), folding endurance (279.3±9.39), moisture uptake (7.06±1.75%), moisture content (6.81±2.34 %) and stable formula.
Conclusion: Therefore, transdermal patches were considered to be potentially suitable for the sustained release of drugs to improve patient compliance.
Keywords: Transdermal patch, Nanosuspension, Rosuvastatin, Fourier transformation infrared spectroscopy, folding endurance, in-vitro drug permeation.
Graphical Abstract
[http://dx.doi.org/10.1016/j.ijpharm.2006.02.045] [PMID: 16580159]
[http://dx.doi.org/10.1211/0022357023691] [PMID: 15233860]
[http://dx.doi.org/10.3390/pharmaceutics9030033] [PMID: 28878145]
[http://dx.doi.org/10.1155/2009/956712]
[http://dx.doi.org/10.1016/S0149-2918(03)80316-8] [PMID: 14667956]
[http://dx.doi.org/10.2147/VHRM.S3662] [PMID: 19436657]
[http://dx.doi.org/10.22159/ijcpr.2017.v9i3.19584]
[http://dx.doi.org/10.1111/bph.13059] [PMID: 25560046]
[http://dx.doi.org/10.22270/ijdra.v1i3.115]
[http://dx.doi.org/10.1016/j.jcis.2016.09.003] [PMID: 27657837]
[http://dx.doi.org/10.3389/fbioe.2018.00015] [PMID: 29497609]
[http://dx.doi.org/10.1007/s11120-009-9439-x] [PMID: 19513810]
[http://dx.doi.org/10.22159/ajpcr.2019.v12i11.35670]
[http://dx.doi.org/10.3390/pharmaceutics11110609] [PMID: 31766305]
[http://dx.doi.org/10.1080/17458080.2015.1055841]
[http://dx.doi.org/10.5958/0974-360X.2020.00841.0]
[http://dx.doi.org/10.1186/s40543-016-0105-6]
[PMID: 15684489]
[PMID: 20524422]
[http://dx.doi.org/10.1081/DIS-120015368]
[http://dx.doi.org/10.1016/j.nano.2008.01.003] [PMID: 18339584]
[http://dx.doi.org/10.1016/B978-0-12-416020-0.00007-3] [PMID: 22093222]
[http://dx.doi.org/10.1093/toxsci/kfm240] [PMID: 17872897]
[http://dx.doi.org/10.1070/RC2013v082n01ABEH004329]
[http://dx.doi.org/10.4103/2231-4040.82950] [PMID: 22171298]
[http://dx.doi.org/10.1038/s41598-017-02523-4] [PMID: 28536446]
[http://dx.doi.org/10.37285/ijpsn.2009.2.1.10]
[http://dx.doi.org/10.1016/j.mee.2007.12.067]
[http://dx.doi.org/10.1016/S0169-409X(01)00113-2] [PMID: 11369080]
[http://dx.doi.org/10.22270/jddt.v3i4.590]
[http://dx.doi.org/10.21276/irjps.2017.4.2.3]
[http://dx.doi.org/10.1016/j.bfopcu.2018.04.001]