Development and evaluation of TPGS/PVA-based nanosuspension for enhancing dissolution and oral bioavailability of ticagrelor

Na, Young-Guk; Pham, Thi Mai Anh; Byeon, Jin‐Ju; Kim, Min-Ki; Han, Min-Gu; Baek, Jong-Suep; Lee, Hong-Ki

doi:10.1016/j.ijpharm.2020.119287

Cited by 34 publications

(14 citation statements)

References 45 publications

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“…First, MMs and MNs increase the dissolution by decreasing particle size, providing better absorption and permeation of magnolol. In addition, the nanosized particles can improve paracellular and intracellular transports, thereby increasing the intestinal absorption and protecting against drug degradation by enteric enzymes (Yun et al, 2013;Na et al, 2020). MNs provides an immediate release of drug contributed to smaller T max and high C max .…”

Section: Discussionmentioning

confidence: 99%

“…MNs provides an immediate release of drug contributed to smaller T max and high C max . The improved bioavailability of magnolol in MNs can be ascribed to the presence of surfactants and stabilizers, which increases the apparent solubility, as well as to particle size reduction leading to amplified surface area (Mori et al., 2016 ; Nagaraj et al., 2017 ). This induces immediate drug release, making more drugs available at the absorption site.…”

Section: Discussionmentioning

confidence: 99%

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Enhanced oral bioavailability of magnolol via mixed micelles and nanosuspensions based on Soluplus ^® -Poloxamer 188

Yong-chun

et al. 2020

Drug Delivery

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Magnolol, known to have extensive biological activities, is the major bioactive ingredient isolated from the root and stem bark of Magnolia officinalis. However, the clinical application of magnolol is limited by poor aqueous solubility and absorption. The aim of this study is to develop novel mixed micelles and nanosuspensions composed of two biocompatible copolymers, Soluplus V R and Poloxamer 188, and to improve the solubility and oral bioavailability of magnolol. The magnolol-loaded mixed micelles (MMs) and magnolol nanosuspensions (MNs) were prepared to use film hydration and antisolvent methods, respectively. The optimal MMs and MNs formulations were prepared to use magnolol, Soluplus V R , and Poloxamer 188 in ratios of 1:12:5 and 2:1:1, respectively. The average particle size of MMs was 111.8 ± 14.6, and MNs was 78.53 ± 5.4 nm. The entrapment and drug loading efficiency for MMs were 89.58 ± 2.54% and 5.46 ± 0.65%, correspondingly. The drug loading efficiency of MNs was 42.50 ± 1.57%. In the in vitro release study, MMs showed a slow drug release while that of MNs was fast. The results of the Caco-2 transcellular transport study indicated that both MMs and MNs increased the permeation of magnolol. MMs and MNs markedly promoted gastrointestinal drug absorption by 2.85 and 2.27-fold, respectively, as shown in the pharmacokinetics study. These results indicated that both MMs and MNs formulations prepared with Soluplus V R and Poloxamer 188 are promising drug delivery systems for improving the oral absorption of insoluble drugs in the gastrointestinal tract.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Enhanced oral bioavailability of magnolol via mixed micelles and nanosuspensions based on Soluplus ^® -Poloxamer 188

Yong-chun

et al. 2020

Drug Delivery

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“…Non-everted gut sac models are usually performed to investigate drug permeability through the GI membrane. The experiment was carried out by modifying the previously reported method [ 23 , 24 ]. Briefly, rats ( n = 4 for each group) were sacrificed by injecting CO 2 gas and then incised in the middle of the abdomen.…”

Section: Methodsmentioning

confidence: 99%

Development and Evaluation of Docetaxel-Phospholipid Complex Loaded Self-Microemulsifying Drug Delivery System: Optimization and In Vitro/Ex Vivo Studies

et al. 2020

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Docetaxel (DTX) has clinical efficacy in the treatment of breast cancer, but it is difficult to develop a product for oral administration, due to low solubility and permeability. This study focused on preparing a self-microemulsifying drug delivery system (SME) loaded with DTX-phospholipid complex (DTX@PLC), to improve the dissolution and gastrointestinal (GI) permeability of DTX. A dual technique combining the phospholipid complexation and SME formulation described as improving upon the disadvantages of DTX has been proposed. We hypothesized that the complexation of DTX with phospholipids can improve the lipophilicity of DTX, thereby increasing the affinity of the drug to the cell lipid membrane, and simultaneously improving permeability through the GI barrier. Meanwhile, DTX@PLC-loaded SME (DTX@PLC-SME) increases the dissolution and surface area of DTX by forming a microemulsion in the intestinal fluid, providing sufficient opportunity for the drug to contact the GI membrane. First, we prepared DTX@PLC-SME by combining dual technologies, which are advantages for oral absorption. Next, we optimized DTX@PLC-SME with nanosized droplets (117.1 nm), low precipitation (8.9%), and high solubility (33.0 mg/g), which formed a homogeneous microemulsion in the aqueous phase. Dissolution and cellular uptake studies demonstrated that DTX@PLC-SME showed 5.6-fold higher dissolution and 2.3-fold higher DTX uptake in Caco-2 cells than raw material. In addition, an ex vivo gut sac study confirmed that DTX@PLC-SME improved GI permeability of DTX by 2.6-fold compared to raw material. These results suggested that DTX@PLC-SME can significantly overcome the disadvantages of anticancer agents, such as low solubility and permeability.

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“…The three factors were set as the amount of SDS (X 1 ), the amount of PVP/VA (X 2 ), and the volume of the aqueous phase (X 3 ), respectively. The amount of SDS (X 1 ) and PVP/VA (X 2 ) affects the solubility of CUR and the adequate steric repulsion to cover the entire surface of the nanoparticle, respectively [29]. Moreover, the volume of aqueous phase (X 3 ) could change the viscosity of the formulation.…”

Section: Optimization Of Cur-nspmentioning

confidence: 99%

“…Narrow and homogeneous size distribution (Y 2 ) of the nanoparticle could affect the stability and efficiency of CUR-NSP [32]. Furthermore, the low precipitation (Y 3 ) of nanoparticle indicates that large amount of drug is encapsulated in the NSP [29].…”

Section: Optimization Of Cur-nspmentioning

confidence: 99%

Development and Evaluation of Tannic Acid-Coated Nanosuspension for Enhancing Oral Bioavailability of Curcumin

Lee

Bang

et al. 2021

Pharmaceutics

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Curcumin (CUR) has been used in the treatment of various diseases such as cough, fever, skin disease, and infection because of various biological benefits such as anti-inflammatory, antiviral, antibacterial, and antitumor activity. However, CUR is a BCS class 4 group and has a limitation of low bioavailability due to low solubility and permeability. Therefore, the purpose of this study is to prepare a nanosuspension (NSP) loaded with CUR (CUR-NSP) using a statistical design approach to improve the oral bioavailability of CUR, and then to develop CUR-NSP coated with tannic acid to increase the mucoadhesion in the GI tract. Firstly, the optimized CUR-NSP, composed of sodium dodecyl sulfate (SDS) and polyvinylpyrrolidone/vinyl acetate (PVP/VA), was modified with tannic acid (TA). The particle size and polydispersity index of the formulation measured by laser scattering analyzer were 127.7 ± 1.3 nm and 0.227 ± 0.010, respectively. In addition, the precipitation in distilled water (DW) was 1.52 ± 0.58%. Using a differential scanning calorimeter and X-ray diffraction analysis, the stable amorphous form of CUR was confirmed in the formulation, and it was confirmed that CUR-NSP formulation was coated with TA through a Fourier transform-infrared spectroscopy. In the mucoadhesion assay using the turbidity, it was confirmed that TA-CUR-NSP had higher affinity for mucus than CUR-NSP under all pH conditions. This means that the absorption of CUR can be improved by increasing the retention time in the GI tract of the formulation. In addition, the drug release profile showed more than 80% release, and in the cellular uptake study, the absorption of the formulation (TA-CUR-NSP) containing TA acting as an inhibitor of P-gp was increased by 1.6-fold. In the evaluation of antioxidant activity, the SOD activity of TA-CUR-NSP was remarkably high due to TA, which improves cellular uptake and has antioxidant activity. In the pharmacokinetic evaluation, the maximum drug plasma concentration of the TA-coated NSP formulation was 7.2-fold higher than that of the pure drug. In all experiments, it was confirmed that the TA-CUR-NSP is a promising approach to overcome the low oral bioavailability of CUR.

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Development and evaluation of TPGS/PVA-based nanosuspension for enhancing dissolution and oral bioavailability of ticagrelor

Cited by 34 publications

References 45 publications

Enhanced oral bioavailability of magnolol via mixed micelles and nanosuspensions based on Soluplus ^® -Poloxamer 188

Enhanced oral bioavailability of magnolol via mixed micelles and nanosuspensions based on Soluplus ^® -Poloxamer 188

Development and Evaluation of Docetaxel-Phospholipid Complex Loaded Self-Microemulsifying Drug Delivery System: Optimization and In Vitro/Ex Vivo Studies

Development and Evaluation of Tannic Acid-Coated Nanosuspension for Enhancing Oral Bioavailability of Curcumin

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Development and evaluation of TPGS/PVA-based nanosuspension for enhancing dissolution and oral bioavailability of ticagrelor

Cited by 34 publications

References 45 publications

Enhanced oral bioavailability of magnolol via mixed micelles and nanosuspensions based on Soluplus ® -Poloxamer 188

Enhanced oral bioavailability of magnolol via mixed micelles and nanosuspensions based on Soluplus ® -Poloxamer 188

Development and Evaluation of Docetaxel-Phospholipid Complex Loaded Self-Microemulsifying Drug Delivery System: Optimization and In Vitro/Ex Vivo Studies

Development and Evaluation of Tannic Acid-Coated Nanosuspension for Enhancing Oral Bioavailability of Curcumin

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Product

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Enhanced oral bioavailability of magnolol via mixed micelles and nanosuspensions based on Soluplus ^® -Poloxamer 188

Enhanced oral bioavailability of magnolol via mixed micelles and nanosuspensions based on Soluplus ^® -Poloxamer 188