The preparation and physicochemical characterization of eprosartan mesylate-laden polymeric ternary solid dispersions for enhanced solubility and dissolution rate of the drug

Abstract

Background. Eprosartan mesylate is a poorly water-soluble drug. It does not dissolve well in the aqueous gastrointestinal fluid, which means it is not absorbed well via the oral route, because a drug can cross cell membranes when it is dissolved in the gastrointestinal fluid. Objectives. The purpose of this research was to enhance the aqueous solubility and dissolution rate of eprosartan mesylate using the solid dispersion technique. Enhancing the solubility and dissolution leads to better absorption via the oral route. Material and methods. A number of eprosartan mesylate-laden polymeric solid dispersions were prepared with hydroxypropyl methylcellulose (HPMC) and polysorbate 80 by means of the solvent evaporation technique. The impact of the weight ratios of the constituents on the solubility and dissolution rate was studied in comparison with the plain drug. The formulation presenting the optimal solubility and dissolution underwent the solid-state characterization using X-ray diffraction (XRD), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), and Fourier-transform infrared spectroscopy (FTIR). Results. Both polysorbate 80 and HPMC positively affected the solubility and dissolution of eprosartan mesylate. Conclusions. In particular, a ternary solid dispersion consisting of eprosartan mesylate, HPMC and polysorbate 80 at a weight ratio of 1:4.2:0.3 showed the highest solubility (36.39 ± 3.95 mg/mL) and dissolution (86.19 ±4.09% in 10 min). Moreover, the drug was present in the amorphous form in the solid dispersion with no covalent drug-excipient interactions.

Formulation and characterization of eprosartan mesylate and β-cyclodextrin inclusion complex prepared by microwave technology

“…The peak corresponding to CO, SO 2 , and O–H group is found at 1696 cm –1 , 1210 cm –1 , and 1421, respectively ( Figure 8(A) ). These peaks are in agreement with the previously reports (Bhandaru et al., 2015 ; Dangre et al., 2016 ; Yousaf et al., 2018 ; Shekhawat & Pokharkar, 2019 ; Tekko et al., 2019 ).…”

“…Further, the data obtained were implemented to various release kinetic models for each sample (Bhandaru et al., 2015 ; Dangre et al., 2016 ; Yousaf et al., 2018 ; Reddy, 2019 ).…”

“…Since the oral bioavailability was found only 13%, hence a high dose of drug may be required for an efficient management of hypertension. Since the oral bioavailability of EM is circumscribed by the solubility, hence the improvement in the EM aqueous solubility could advance its oral efficaciousness and lessening the need for such high doses (Yousaf et al., 2018 ). Accordingly, there is a demand for a formulation that increases the bioavailability of EM.…”

“…Amid the numerous available CDs, β-CD are the inexpensive and are harmless for oral use (Redenti et al., 2001 ; Hirlekar & Kadam, 2009 ). As CDs are comparatively more water-soluble and EM could establish inclusion complex with CD, and that can formed complex could improve the solubility of the attached EM (Quader et al., 2017 ; Yousaf et al., 2018 ). All the above information intensely encourages us to study the possibility of using β-CD as a carrier to ameliorate the solubility of poorly water soluble drug EM.…”

<p>Electrosprayed Polymeric Nanospheres for Enhanced Solubility, Dissolution Rate, Oral Bioavailability and Antihyperlipidemic Activity of Bezafibrate</p>

“…19,37 That is the why, the formulations VI and VII with higher polymer concentrations showed apparently decreased solubility of bezafibrate. 37,38 Formulation V, consisting of bezafibrate, PVP K30 and cremophor ELP (1/12/1.5, w/w/w), showed apparently the highest solubility of bezafibrate (27.59 ± 4.90 mg/mL) which was about fivefold than that of the corresponding physical mixture. The physical mixture was obtained by simply triturating bezafibrate, PVP K30 and cremophor ELP (1/12/1.5, w/w/w) using a pestle and mortar.…”