Cefdinir Solid Dispersion Composed of Hydrophilic Polymers with Enhanced Solubility, Dissolution, and Bioavailability in Rats

Abstract

The aim of this work was to develop cefdinir solid dispersions (CSDs) prepared using hydrophilic polymers with enhanced dissolution/solubility and in vivo oral bioavailability. CSDs were prepared with hydrophilic polymers such as hydroxypropyl-methylcellulose (HPMC; CSD1), carboxymethylcellulose-Na (CMC-Na; CSD2), polyvinyl pyrrolidone K30 (PVP K30; CSD3) at the weight ratio of 1:1 (drug:polymer) using a spray-drying method. The prepared CSDs were characterized by aqueous solubility, differential scanning calorimetry (DSC), powder X-ray diffraction (p-XRD), scanning electron microscopy (SEM), aqueous viscosity, and dissolution test in various media. The oral bioavailability of CSDs was also evaluated in rats and compared with cefdinir powder suspension. The cefdinir in CSDs was amorphous form, as confirmed in the DSC and p-XRD measurements. The developed CSDs commonly resulted in about 9.0-fold higher solubility of cefdinir and a significantly improved dissolution profile in water and at pH 1.2, compared with cefdinir crystalline powder. Importantly, the in vivo oral absorption (represented as AUCinf) was markedly increased by 4.30-, 6.77- and 3.01-fold for CSD1, CSD2, and CSD3, respectively, compared with cefdinir suspension in rats. The CSD2 prepared with CMC-Na would provide a promising vehicle to enhance dissolution and bioavailability of cefdinir in vivo.

Construction and Evaluation of Composite Scaffold Properties of Cellulose Base Enhanced with Calcium Alginate Containing Propolis for Use in Skin Tissue Engineering

“…In general, if the contact angle of the scaffold is more than 90 0 , the surface is hydrophobic, and if it is less than 90 0 , the surface of scaffold is called hydrophilic [22]. Since CMC is a hydrophilic polymer [23] it is expected that by adding calcium alginate to the scaffold, the water contact angle is also increased, the results of this analysis confirmed this statement. With the addition of propolis extract, the contact angle of the scaffold was reached 23.87 0 , indicating lower water content.…”

Polyelectrolytes in Hot Melt Extrusion: A Combined Solvent-Based and Interacting Additive Technique for Solid Dispersions

“…NaCMC was recently extruded with polydimethylsiloxane as a polymeric mixture to form material for 3D printing [12] or it is occasionally used in spray drying [13]. The polymer shows good water solubility and extensive swelling behavior, which are both interesting properties for a new modified matrix produced by HME.…”

Application of Spray Drying Particle Engineering to a High-Functionality/Low-Solubility Milk Thistle Extract: Powders Production and Characterization

“…A way to enhance the absorption after the oral administration as well as, targeted biological efficacy is to produce technological delivery systems able to improve dissolution and permeation rate of the active ingredient [ 2 , 3 ]. Numerous delivery systems had been developed and studied extensively in oral drug delivery [ 4 , 5 , 6 ], but the application of this research area to nutraceuticals only is emerging very recently [ 7 , 8 , 9 , 10 , 11 , 12 ]. The milk thistle ( Silybum marianum (L.) Gaertn, Asteraceae), extract is an essential source of silymarin; it is a well-known complex of flavonolignans (silybin A and B, isosilybin A and B, silydianin, and silychristin) and flavonoids (taxifolin and quercetin) used to treat a variety of ailments like liver (hepatitis, cirrhosis, and icterus), kidney, and gallbladder problems [ 13 , 14 ].…”