Abstract
Andrographolide (AG), a major diterpene lactone isolated from Andrographis paniculata (Burm. f.) Nees (Acanthaceae), possesses a wide spectrum of biological activities. However, its poor water solubility and low bioavailability limit its clinical application. Therefore, this study aimed to develop a solid dispersion (SD) formulation to increase the aqueous solubility and dissolution rate of AG. Different drug-polymer ratios were used to prepare various SDs. The optimized formulation was characterized for differential scanning calorimetry, Fourier transform infrared spectroscopy, and powder X-ray diffraction. The analysis indicated that the optimized SD enhanced AG solubility and dissolution rates by changing AG crystallinity to an amorphous state. The dissolution behaviors of the optimum SD composed of an AG-polyvinylpyrrolidone K30-Kolliphor EL ratio of 1:7:1 (w/w/w) resulted in the highest accumulated dissolution (approximately 80%). Pharmacokinetic studies revealed that Cmax/dose and the AUC/dose increased by 3.7-fold and 3.0-fold, respectively, compared with AG suspension. Furthermore, pretreatment using the optimized AG-SD significantly increased the swimming time to exhaustion by 1.7-fold and decreased the plasma ammonia level by 71.5%, compared with the vehicle group. In conclusion, the optimized AG-SD formulation appeared to effectively improve its dissolution rate and oral bioavailability. Moreover, the optimized AG-SD provides a promising treatment against physical fatigue.
Highlights
Andrographis paniculata (Burm. f.) Nees (Acanthaceae) is a medicinal plant native to south Asia and India
Several studies have discovered the pharmacological activities of AG, and these findings demonstrated that AG might have potential for the alleviation of several diseases caused by the oxidative stress, and the main mechanisms include the activation of nuclear factor erythroid-2-related factor 2 and inhibition of nuclear factor-κB activation [2,3,4]
The dissolution profile revealed that the solid dispersion (SD) made of PVP generally exhibited a quicker release than SD made of polyethylene glycol (PEG) 6000 (Figure 1a)
Summary
Andrographis paniculata (Burm. f.) Nees (Acanthaceae) is a medicinal plant native to south Asia and India. A. paniculata (AP) has a very bitter taste and is traditionally applied to ease internal heat, pain, and inflammation according to Chinese medicinal theory [1]. Several studies have discovered the pharmacological activities of AG, and these findings demonstrated that AG might have potential for the alleviation of several diseases caused by the oxidative stress, and the main mechanisms include the activation of nuclear factor erythroid-2-related factor 2 and inhibition of nuclear factor-κB activation [2,3,4]. Recent studies have demonstrated that antioxidant supplementation may serve as a practical strategy for the alleviation of physical fatigue through modulating oxidative stress and inflammation status [5,6,7]. Proposing a practical delivery system for increasing the oral bioavailability of AG remains crucial for the successful clinical and health application of this active component
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