Impact of porous microsponges in minimizing myotoxic side effects of simvastatin

Abstract

Simvastatin (SV) is a poorly soluble drug; its oral administration is associated with a significant problem: Myopathy. The present study aims to formulate SV microsponges that have the potential to minimize the myotoxicity accompanying the oral administration of the drug. SV microsponges were prepared by exploiting the emulsion solvent evaporation technique. The % entrapment efficiency (%EE) of the drug approached 82.54 ± 1.27%, the mean particle size of SV microsponges ranged from 53.80 ± 6.35 to 86.03 ± 4.79 µm in diameter, and the % cumulative drug release (%CDR) of SV from microsponges was significantly higher than that from free drug dispersion much more, the specific surface area of the optimized microsponges formulation was found to be 16.6 m2/g revealed the porosity of prepared microsponges. Histological and glycogen histochemical studies in the skeletal muscles of male albino rats revealed that microsponges were safer than free SV in minimizing myotoxicity. These findings were proven by Gene expression of Mitochondrial fusion and fission (Mfn1) & (Fis1) and (Peroxisome proliferator-activated receptor gamma co-activator 1α) PGC-1α. Finally, our study ascertained that SV microsponges significantly decreased the myotoxicity of SV.

Mitochondrial Fission as a Therapeutic Target for Metabolic Diseases: Insights into Antioxidant Strategies

“…Some studies have reported that statin treatment can reduce the expression and activity of the mitochondrial fission proteins Drp1 and Fis1 [ 214 , 215 , 216 ]. However, the results from different studies are conflicting, with some reporting an increase in fission-related proteins/mitochondrial dysfunction and others showing no significant effect of statin treatment [ 213 , 217 , 218 , 219 ]. It is likely that the effects of statins on mitochondrial dynamics vary depending on the specific statin, its dosage, the duration of treatment, and the experimental model or tissue studied.…”

Advancements in microsponges for the management of vaginal and colorectal diseases: A comprehensive review

“…Microsponges porous nature provides a number of benefits in drug delivery, including controlled release, increased bioavailability, drug protection, targeted delivery, reduced side effects, and taste masking. Because of these characteristics, microsponges are a diverse and useful platform for refining drug formulations and increasing therapeutic effects [4] Research utilizing mitiglinide microsponges for prolonged drug release was prepared via quasi-emulsion solvent diffusion technique. The particle size of the microsponges was found to be ranging between 39.15-215.78 µm with an entrapment efficiency of 76.7 − 98.74% ± 1.37.…”

“…Sustain drug release of microsponges is associated with the increased bioavailability of drugs [9] . Microsponges can be employed to incorporate solids and liquids/ oils, which are thermally (up to 130 °C ), physically and chemically stable (pH range of [1][2][3][4][5][6][7][8][9][10][11] without the use of preservatives [10][11][12][13] .…”