Abstract:A well-controlled release of TAK-029, a water-soluble neutral drug, with small initial burst was achieved by utilizing its amorphous form as a result of possible interaction with PLGA and L-arginine.
“…Decreased burst release in microspheres is beneficial for forming a uniform amorphous state of ASM within the PLGA carriers. (Takada et al., 1997 ). The DSC data in Figure 2(B) show that ASM produced an endothermic peak at about 146 °C, similar to its melting point.…”
“…Decreased burst release in microspheres is beneficial for forming a uniform amorphous state of ASM within the PLGA carriers. (Takada et al., 1997 ). The DSC data in Figure 2(B) show that ASM produced an endothermic peak at about 146 °C, similar to its melting point.…”
“…Microspheres (300 mg) were loaded in a dialysis bag, which was placed in the above release media. To determine the drug release behavior accurately, the remaining microspheres were recovered by centrifugation at the specified points in time: 0, 2, 4,6,8,10,1215,17,18,20,22, and 24 h. The amount of OTA remaining in the microspheres was also determined by HPLC as mentioned above. The correlation between the longterm release (the FT method) and the accelerated release was established by plotting different levels of release in days versus hours.…”
Section: Accelerated Release Studies Using the Paddle Methodsmentioning
ABSTRACT:In this study, octreotide acetate (OTA)-loaded poly(lactide-co-glycolide) (PLGA) microspheres were prepared using an optimized double emulsion solvent evaporation method. The loading capacity (LC) was increased by raising the concentration of OTA in the inner aqueous phase (W1), and burst release was decreased (<10.0%) because the higher viscosity hindered the diffusion of OTA. The in vitro release profiles were closely correlated with in vivo release profiles calculated using the Wagner-Nelson method (r = 0.9876). To evaluate the drug release profiles rapidly, an accelerated release method was developed. In the accelerated release method, the acidic and alkaline buffers (the first 6 h, pH 4.0; the last 18 h, pH 9.6) were used as release media, respectively. Results indicated that the accelerated release profiles (24 h) were closely correlated with the in vivo release profiles (r = 0.9623). Therefore, through optimization of the experiment variables (buffer components and pH), an accelerated release method was developed to evaluate in vivo drug release from microspheres. C
“…The solid state of hydrophilic drug can greatly aid in preventing drug leakage caused due to anionic surfactant [ 32 ]. This method can effectively entrap sensitive materials with lesser damage and higher entrapment efficiency [ 40 – 42 ]. Fig.…”
An emulsion is a biphasic dosage form comprising of dispersed phase containing droplets that are uniformly distributed into a surrounding liquid which forms the continuous phase. An emulsifier is added at the interface of two immiscible liquids to stabilize the thermodynamically unstable emulsion. Various types of emulsions such as water-in-oil (w-o), oil-in-water (o-w), microemulsions, and multiple emulsions are used for delivering certain drugs in the body. Water (aqueous) phase is commonly used for encapsulating proteins and several other drugs in water-in-oil-in-water (w-o-w) emulsion technique. But this method has posed certain problems such as decreased stability, burst release, and low entrapment efficiency. Thus, a novel “solid-in-oil-in-water” (s-o-w) emulsion system was developed for formulating certain drugs, probiotics, proteins, antibodies, and tannins to overcome these issues. In this method, the active ingredient is encapsulated as a solid and added to an oil phase, which formed a solid-oil dispersion. This dispersion was then mixed with water to form a continuous phase for enhancing the drug absorption. This article focuses on the various studies done to investigate the effectiveness of formulations prepared as solid-oil-water emulsions in comparison to conventional water-oil-water emulsions. A summary of the results obtained in each study is presented in this article. The s-o-w emulsion technique may become beneficial in near future as it has shown to improve the stability and efficacy of the entrapped active ingredient.
Graphical abstract
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