Metformin hydrochloride sustained release biopolymeric system composed by PLLA‐CMC microparticles

Abstract

Metformin hydrochloride (MetHCl) is a drug extensively used to treat diabetes mellitus Type 2. However, its high hydrophilicity drastically reduces its metabolic absorption. Consequently, high drug concentrations should be taken by patients to achieve the desired therapeutical efficiency, causing several side effects. The present study proposes the development of a MetHCl sustained release biopolymeric system composed of poly(L-lactic acid) (PLLA) and carboxymethyl cellulose (CMC) as a strategy to minimize the problems aforementioned. The PLLA-CMC microparticles were produced by the double emulsion-solvent evaporation technique using two distinct emulsifiers in the first emulsion (Span 80 and Tween 80). The microparticles were characterized by ultraviolet-visible spectrophotometry, scanning electron microscopy with field emission gun, thermogravimetric analyses, and differential scanning calorimetry (DSC). Additionally, in vitro drug release assays were performed. The results demonstrated that the emulsion stability and encapsulation efficiency increased in a dependent fashion way with the CMC concentration. DSC findings showed that the choice of the emulsifier of the first emulsion influences the polymer particle's crystallinity and, consequently, the releasing behavior of the drug. The in vitro studies revealed that the encapsulation of MetHCl in PLLA-CMC microparticles is a promising sustained release system compatible with a zero-order kinetic mechanism.

The Antidiabetic Activities of Neocryptotanshinone: Screened by Molecular Docking and Related to the Modulation of PTP1B

“…Our study proves the hypoglycemic efficacy of NCTS. Comparatively, chronic and high-dose administration with Met may show side effects on the gastrointestinal tract [ 42 ], and its high hydrophilicity leads to a reduced degree of metabolic absorption and insufficient bioavailability [ 43 , 44 ]. However, the security of NCTS needs further investigation.…”

Biodegradable Gg-cl-poly(NIPAm-co-AA)/-o-MWCNT based hydrogel for combined drug delivery system of metformin and sodium diclofenac: in vitro studies

“…This behavior is a concern of the high hydrophilicity of the drug. 15 Various kinetic models are tted using the release data. These models working equations are listed in Table 3.…”

“…This drug is usually given to people whose glucose levels cannot be managed via diet and exercise. 15 It has three basic functions: reducing sugar absorption in the small intestine, stopping the liver from excreting more glucose into the blood, and eventually supporting the body in using natural insulin properly. As a result, it reduces endogenous glucose synthesis while causing no obvious hypoglycemia.…”

Formulation and Evaluation of Xanthan Gum Microspheres for the Sustained Release of Metformin Hydrochloride

“…Another study was conducted by Nath et al [ 19 ] on the development of floating microcapsules for metformin hydrochloride based on Eudragit RL 100 and cellulose acetate butyrate by the nonaqueous emulsion–solvent evaporation method. Silva et al [ 20 ] used poly(L-lactic acid) and carboxymethyl cellulose microparticles produced by the double emulsion–solvent evaporation technique for MTH sustained release. Furthermore, Choudhury et al [ 21 ] prepared cellulose acetate microspheres by emulsion–solvent evaporation for metformin hydrochloride’s gastric retention.…”