Cardioprotective Efficacy of Silymarin Liquisolid in Isoproterenol Prompted Myocardial Infarction in Rats

Abstract

Myocardial infarction (MI) is the principal cause of death in many countries. Silymarin (SM) is a herbal antioxidant and can be efficiently used in preventing cardiovascular diseases (CVDs). The study is aimed to enhance the absorption rate and biological activity of SM by using liquisolids besides investigating the cardioprotective activity of SM and its selected liquisolid formula against isoproterenol prompted cardiotoxicity in rats. Eight formulae were prepared according to (2 3 ) full-factorial design. The effect of viscosity increasing agent type and concentration, as well as the carrier/coat ratio on the dissolution rate and angle of repose were studied. All formulae were tested for content uniformity, micromeritic properties, dissolution performance besides the evaluation of its physicochemical properties, and scanning electron microscopy (SEM). Based on the factorial design outcomes, the highest desirability was obtained from F3 with excipient ratio value (R) of 20%, dissolution rate at Q 5 min of 26.9%, and angle of repose of 19. Oral administration of F3 liquisolid and SM revealed a significant protective efficacy against the modification of cardiac plasma markers, brain natriuretic peptide (BNP), interleukin-10 (IL-10), vascular endothelial growth factor (VEGF), and transforming growth factor (TGF)-β1 besides cardiac superoxide dismutase (SOD), malondialdehyde (MDA), and total protein kinase-1 (Akt-1) levels. Additionally, they minimized cardiac inducible nitric oxide synthase (iNOS), microRNA-34a (miR-34a), and p38 mitogen-activated protein kinase (p38-MAPK) levels. In conclusion, F3 liquisolid compact possessed an overall pronounced results over pure SM reckoned to its enhanced solubility and efficacy.

Recent Progress in Environmental Toxins-Induced Cardiotoxicity and Protective Potential of Natural Products

“…Silibinin is a polyphenolic flavonoid extracted from the seeds of milk thistle ( Verdura et al, 2018 ), possessing strong antioxidant and cardioprotective activities ( Sheta et al, 2020 ). It has been successfully employed as a protective agent against arsenic-induced in vivo model of hepatotoxicity ( Muthumani and Prabu, 2012 ).…”

Fabrication and Evaluation of Celecoxib Oral Oleogel to Reduce the Inflammation of Ulcerative Colitis

“…The oleogel preparation was left aside for 48 h at room temperature to accomplish equilibrium, at this point the crystals begin to be formed through the oil (30). Half gram of each system was packed into the hard gelatin capsule (32) size 00 (33)(34)(35). No leakage was detected from all capsules packed with the various prepared Celecoxib formulae.…”

Liquisolid systems: Evaluation of the influence of formulation variables on the optimum liquid load

“…However, this technology has gained increased research interest more recently, and during the last decade enhanced dissolution from LS systems has been reported for various poorly soluble drugs (3)(4)(5)(6)(7)(8). Furthermore, recently reported in vivo studies showed improved bioavailability in the case of LS systems with different poorly soluble drugs (9)(10)(11)(12)(13)(14)(15).…”

“…For the industrial application of LS technology in tablet production it is of outmost importance to identify the factors affecting both flowability and compaction properties. The influence of different formulation variables, including the carrier and coating material type, the amount and type of liquid phase, the amount and type of viscosity increasing agent, and carrier to coating ratio, on flow properties and flowable liquid load of LS systems has been intensively investigated over the past years (9,10,(18)(19)(20)(21). For the application of this technology in tablet production not only good flowability, but also acceptable compaction properties have to be ensured.…”