Enhancing the solubility and bioavailability of poorly water-soluble drugs using supercritical antisolvent (SAS) process

Abuzar, Sharif Md; Hyun, Sang Min; Kim, Jun Hee; Park, Hee-Jun; Kim, Min Soo; Park, Jeong Sook; Hwang, Sung Joo

doi:10.1016/j.ijpharm.2017.12.041

Cited by 162 publications

(74 citation statements)

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“…25 To achieve the maximum bioavailability, drug solubility is one of the primary factors that can increase the drug bioavailability. 26 Currently, nanoparticle drug delivery systems are the most commonly used technique for nanomedicine-mediated treatment of diseases. Their nanosize can enhance solubility by providing a large surface area, which increases the penetration rate into a cell membrane and provides a controlled release system with passive or active targeting.…”

Section: Introductionmentioning

confidence: 99%

<p>Nanoparticle Drug Delivery Systems for α-Mangostin</p>

Wathoni¹,

Rusdin²,

Motoyama³

et al. 2020

NSA

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α-Mangostin, a xanthone derivative from the pericarp of Garcinia mangostana L., has numerous bioactivities and pharmacological properties. However, α-mangostin has low aqueous solubility and poor target selectivity in the human body. Recently, nanoparticle drug delivery systems have become an excellent technique to improve the physicochemical properties and effectiveness of drugs. Therefore, many efforts have been made to overcome the limitations of α-mangostin through nanoparticle formulations. Our review aimed to summarise and discuss the nanoparticle drug delivery systems for α-mangostin from published papers recorded in Scopus, PubMed and Google Scholar. We examined various types of nanoparticles for α-mangostin to enhance water solubility, provide controlled release and create targeted delivery systems. These forms include polymeric nanoparticles, nanomicelles, liposomes, solid lipid nanoparticles, nanofibers and nanoemulsions. Notably, nanomicelle modification increased α-mangostin solubility increased more than 10,000 fold. Additionally, polymeric nanoparticles provided targeted delivery and significantly enhanced the biodistribution of α-mangostin into specific organs. In conclusion, the nanoparticle drug delivery system could be a promising technique to increase the solubility, selectivity and efficacy of α-mangostin as a new drug candidate in clinical therapy.

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Section: Introductionmentioning

confidence: 99%

<p>Nanoparticle Drug Delivery Systems for α-Mangostin</p>

Wathoni¹,

Rusdin²,

Motoyama³

et al. 2020

NSA

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“…However, recently, a melt-adsorption process using supercritical carbon dioxide (SC-CO 2 ) has been introduced by some researchers as a more efficient way to load drugs onto adsorbents [33][34][35][36][37]. SC-CO 2 is the most widely used supercritical fluid because of its mild critical conditions, nontoxicity, non-flammability, and low cost, making it an ideal substitute for organic solvents [38][39][40][41]. Especially, SC-CO 2 can lower the melting temperature and viscosity of materials via its low viscosity and high diffusivity, thus it has been used for the supercritical melt-adsorption (SCMA) method [40][41][42][43][44][45][46][47][48].…”

Section: Introductionmentioning

confidence: 99%

Pharmaceutical Characterization and In Vivo Evaluation of Orlistat Formulations Prepared by the Supercritical Melt-Adsorption Method Using Carbon Dioxide: Effects of Mesoporous Silica Type

Park

Hong

et al. 2020

Pharmaceutics

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Orlistat, an anti-obesity drug, has two critical issues-the first is its low efficacy due to low water solubility and the second is side effects such as oily spotting due to its lipase inhibition. The present study was designed to propose a solution using a formulation with mesoporous silica to simultaneously overcome two issues. Orlistat was loaded onto mesoporous silica by the supercritical melt-adsorption (SCMA) method, using carbon dioxide (CO 2 ). Various types of mesoporous silica were used as adsorbents, and the effects of the pore volume, diameter and particle size of mesoporous silica on the pharmaceutical characteristics were evaluated by various solid-state characterization methods and in vitro and in vivo studies in relation to pharmacological efficacy and the improvement of side effects. The results showed that the pore volume and diameter determine loadable drug amount inside pores and crystallinity. The dissolution was significantly influenced by crystallinity, pore diameter and particle size, and the inhibition of lipase activity was in proportion to the dissolution rate. In vivo studies revealed that the serum triglyceride (TG) concentration was significantly decreased in the group administered amorphous orlistat-loaded Neuisilin ® UFL2 with the highest in vitro dissolution rate and lipase activity inhibition in comparison to the commercial product. Furthermore, oily spotting tests in rats revealed that undigested oil was adsorbed onto mesoporous silica after orlistat was released in the gastro-intestinal tract, and it correlated with in vitro result that oil adsorption capacity was dependent on the surface area of empty mesoporous silica. Therefore, it was concluded that mesoporous silica type plays a major role in determining the pharmaceutical characteristics of orlistat formulation prepared using SCMA with CO 2 for improving the low solubility and overcoming the side effects.

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“…In addition, particle engineering and crystal manipulation could be performed by this method [7,8]. In addition, supercritical fluid techniques have been used for producing small and nanosized particles [9][10][11]. However, preventing the crystal growth is the biggest problem in this process.…”

Section: Introductionmentioning

confidence: 99%