Panax ginseng has been used as an herbal medicine for thousands of years. Most of its pharmacological effects are attributed to its constituent ginsenosides, including 20(S)-25methoxyl-dammarane-3b, 12b, 20-triol (20(S)-25-OCH 3 -PPD), which is one of the protopanaxadiol type ginsenosides. It has been found to exhibit anticancer effects by interacting with multiple pharmacological pathways, such as the Wnt/b-catenin, MDM2, ERK/MAPK, and STAT3 signaling pathways. However, its therapeutic potential could be limited by its low bioavailability mainly due to its low aqueous solubility. Thus, several studies have been conducted on its pharmacokinetics and its delivery systems, so as to increase its oral bioavailability. In this review, comprehensive information on its varying pharmacological pathways in cancer, as well as its pharmacokinetic behavior and pharmaceutical strategies, is provided. This information would be useful in the understanding of its diverse mechanisms and pharmacokinetics as an anticancer drug, leading to the design of superior 20(S)-25-OCH 3 -PPD-containing formulations that maximize its therapeutic potential.
In this study, we aimed to design a highly swellable and mechanically robust matrix tablet (SMT) as a gastroretentive drug-delivery system (GRDDS) capable of improving the dissolution behavior of β-lapachone with low aqueous solubility. For the preparation of SMTs, the cogrinding technique and freeze–thaw method were used to disperse β-lapachone in SMTs in an amorphous state and to enhance the swelling and mechanical properties of SMTs, respectively. As a result, the crystallinity of coground β-lapachone incorporated in the SMTs was found to be considerably decreased; thereby, the dissolution rates of the drug in a simulated gastric fluid could be substantially increased. The SMTs of β-lapachone also demonstrated significantly enhanced swelling and mechanical properties compared to those of a marketed product. The reason for this might be because the physically crosslinked polymeric networks with a porous structure that were formed in SMTs through the freeze–thaw method. In addition, β-lapachone was gradually released from the SMTs in 6 h. Therefore, SMTs of β-lapachone developed in this study could be used as GRDDS with appropriate swelling and mechanical properties for improving the dissolution behavior of hydrophobic drugs such as β-lapachone.
Nanotechnology uses very small molecular and intracellular structures ranging from 1 to 100-nanometer in size to create, employ and qualify materials and devices. It is a well-established branch of science having significant applications in wide range of medicine. It has wide usage in pharmaceutics for targeted delivery of drugs and genes into cells. Various targeted procedures in the animal body have been accomplished using nano instruments, especially nano-robotics. Scientific bodies have also set the status of nanomedicine in health fields especially neurological and cancerous antidotes. Thus, nanoparticles of extremely small size have vast prominence in almost all medical fields for facilitating mankind.
Nanotechnology has opened a new era for scientists and engineers to build nanomaterials with diverse applications. Nowadays, nanotechnology plays a vital rolein each and every sector due to its extraordinary physical and chemical properties. It deals with development and synthesis of variety of nanoparticles (NPs), which ranging from 1 to 100 nm. The major approaches used for the synthesis of NPs are top to bottom and bottom to up which mainly included physical, chemical and biological methodologies. This mini review highlights synthesis of NPs through various approaches specifically targeted biological route.
Quercetin is a flavonoid abundantly present in vegetables and fruits and known to possess therapeutic potentials for the prevention and treatment of different diseases owing to its anti-oxidant, anti-inflammatory, anti-viral, and anticancer activities. 1,2 However, the oral bioavailability of quercetin has been reported to be less than 1% in human because of its low aqueous solubility. 3,4 Nevertheless, based on our neutraceutical market search, numerous commercial products of quercetin have been generally formulated as conventional dosage forms such as tablets and capsules that are not specially designed for enhancing the aqueous solubility and dissolution behavior of quercetin.Various nano-sized pharmaceutical formulations have been investigated to improve the aqueous solubility and dissolution behavior of quercetin, such as liposomes, 5 polymeric micelles, 6 and solid lipid nanoparticles. 7 Among them, liposomes are particularly promising because they can efficiently entrap quercetin in the hydrophobic domain of the lipid bilayer, thereby solubilizing the drug and stabilizing its anti-oxidative activity, which could be easily lost in an aqueous environment. 8 However, liposomes suspended in water may aggregate, fuse each other, and leak the entrapped drug as time progresses due to the dispersion instability of liposomes and the fluidic nature of the lipid bilayer. The physically instable properties of liposomes can lead to significant changes in the in vivo biodistribution, efficacy, and safety of drugs incorporated in liposomes. 9,10 To enhance the physical stability of liposomes, freezedried liposomes have been explored because the undesirable phenomena such as drug leakage, aggregation, and fusion among the liposomes are facilitated in an aqueous environment. Owing to their dried state, the physical stability of freeze-dried liposomes can be maintained substantially longer than liposomes suspended in water. However, liposomes can be physically damaged by ice crystals and aggregated during the freeze-drying procedure, resulting in considerable changes in the membrane structure, particle size, and particle size distribution of liposomes. 11 To stabilize liposomes during lyophilization, diverse lyoprotectants have been exploited. In particular, saccharides have been widely used as lyoprotectants because they can form an amorphous glassy matrix with a high viscosity under a freezing condition and thereby prevent the formation of ice crystals, aggregation, and fusion of liposomes. 12 Thus, in this study we aimed to enhance the physical stability of freeze-dried liposomes loaded with quercetin using four different saccharides such as glucose, lactose, sucrose, and trehalose. The lyoprotectants were selected based on their different glass transition temperatures, 13 which is known to be crucial for the lyoprotective ability. 14 We evaluated the effect of the addition of the saccharides to the liposomal suspension containing quercetin on the physical stability of the liposomes after the freeze-drying and rehydratio...
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