Improvement in Solubility and Absorption of Nifedipine Using Solid Solution: Correlations between Surface Free Energy and Drug Dissolution

Abstract

Ternary solid solutions composed of nifedipine (NDP), amino methacrylate copolymer (AMCP), and polysorbate (PS) 20, 60, or 65 were prepared using a solvent evaporation method. The dissolution profiles of NDP were used to study the effect of the addition of polysorbate based on hydrophilic properties. A solid solution of NDP and AMCP was recently developed; however, the dissolution of NDP was <70%. In the present study, polysorbate was added to improve the dissolution of the drug by altering its hydrophilicity. The suitable formulation contained NDP and AMCP at a ratio of 1:4 and polysorbate at a concentration of 0.1%, 0.3%, or 0.6%. Differential scanning calorimetry and powder X-ray diffraction were used to examine the solid solutions. No peak representing crystalline NDP was observed in any solid solution samples, suggesting that the drug was molecularly dispersed in AMCP. The NDP dissolution from NDP powder and solid solution without PS were 16.82% and 58.19%, respectively. The highest dissolution of NDP of approximately 95.25% was noted at 120 min for the formulation containing 0.6% PS20. Linear correlations were observed between the surface free energy and percentages of dissolved NDP (R2 = 0.7115–0.9315). Cellular uptake across Caco-2 was selected to determine the drug permeability. The percentages of cellular uptake from the NDP powder, solid solution without and with PS20 were 0.25%, 3.60%, and 7.27%, respectively.

Increasing Cellular Uptake and Permeation of Curcumin Using a Novel Polymer-Surfactant Formulation

“…Since C 0 (suspension) (A-B) is correlated to the aqueous solubility of curcumin, this suggests that the apical cellular uptake of curcumin can be affected by solubility. This view was further supported by other published studies, which found a positive correlation between the concentration of the drug dissolved in the donor compartment and the in vitro apical cellular drug uptake of Caco-2 cells [ 89 , 90 ].…”

Electrospun Hybrid Films for Fast and Convenient Delivery of Active Herb Extracts

“…During the past half a century, polymers have acted as a backbone role to support the fast developments of pharmaceutics [1][2][3][4][5][6][7][8], particularly the dosage forms for drug delivery [9][10][11][12][13][14][15][16]. The numbers in which natural and synthetic polymers are introduced into this interdisciplinary field is always increasing [17][18][19][20].…”

“…As a popular electrohydrodynamic atomization (EHDA) method, electrospinning is similar to electrospraying in taking advantage of the easy interactions between working liquids and higher voltage electrostatic energy [56][57][58][59][60][61][62]. Their differences lie in the following: (1) the working fluids utilized in electrospinning often have a higher concentration and related viscosity than those exploited during electrospraying, and correspondingly (2) the products from electrospinning are fibers, whereas those from electrospraying are particles [63][64][65][66][67]. With either electrospinning or electrospraying, the functional ingredients can be co-dissolved with the polymeric matrices to experience the working processes for generating the desired polymer-based composites in a single step and a straightforward manner.…”