A Soluplus/Poloxamer 407-based self-nanoemulsifying drug delivery system for the weakly basic drug carvedilol to improve its bioavailability

Han, Han; Li, Yun; Peng, Zhihua; Long, Kaiqi; Zheng, Chunli; Wang, Weiping; Webster, Thomas J.; Ge, Liang

doi:10.1016/j.nano.2020.102199

Cited by 11 publications

(4 citation statements)

References 42 publications

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“…These findings were comparable to those of various reported studies, where researchers have disclosed that thiolation might not significantly improve the swelling index of certain polymers. Bernkop-Schnürch and his co-worker observed the swelling index of tablets prepared with thiolated and non-thiolated carboxymethyl cellulose, and they revealed that there were no considerable differences in the characteristics of the tablets [ 32 ]. Furthermore, in another study that was based upon the modified and unmodified chitosan, the author statistically evaluated the swelling index by using a Student’s t-test.…”

Section: Discussionmentioning

confidence: 99%

Synthesis and Evaluation of Thiol-Conjugated Poloxamer and Its Pharmaceutical Applications

et al. 2021

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The current study was designed to convert the poloxamer (PLX) into thiolated poloxamer (TPLX), followed by its physicochemical, biocompatibilities studies, and applications as a pharmaceutical excipient in the development of tacrolimus (TCM)-containing compressed tablets. Thiolation was accomplished by using thiourea as a thiol donor and hydrochloric acid (HCl) as a catalyst in the reaction. Both PLX and TPLX were evaluated for surface morphology based on SEM, the crystalline or amorphous nature of the particles, thiol contents, micromeritics, FTIR, and biocompatibility studies in albino rats. Furthermore, the polymers were used in the development of compressed tablets. Later, they were also characterized for thickness, diameter, hardness, weight variation, swelling index, disintegration time, mucoadhesion, and in vitro drug release. The outcomes of the study showed that the thiolation process was accomplished successfully, which was confirmed by FTIR, where a characteristic peak was noticed at 2695.9968 cm−1 in the FTIR scan of TPLX. Furthermore, the considerable concentration of the thiol constituents (20.625 µg/g of the polymer), which was present on the polymeric backbone, also strengthened the claim of successful thiolation. A mucoadhesion test illustrated the comparatively better mucoadhesion strength of TPLX compared to PLX. The in vitro drug release study exhibited that the TPLX-based formulation showed a more rapid (p < 0.05) release of the drug in 1 h compared to the PLX-based formulation. The in vivo toxicity studies confirmed that both PLX and TPLX were safe when they were administered to the albino rats. Conclusively, the thiolation of PLX made not only the polymer more mucoadhesive but also capable of improving the dissolution profile of TCM.

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Section: Discussionmentioning

confidence: 99%

Synthesis and Evaluation of Thiol-Conjugated Poloxamer and Its Pharmaceutical Applications

et al. 2021

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“…These solubilizers are suitable components in the modeling of nanostructured carriers to ensure good solubility of caffeic acid. Caffeic acid has poor bioavailability, so nanostructured carriers are one of the future solutions to improve its penetration through biological membranes [54,55]. In order to more fully understand their effect on the solubility of caffeic acid, a dissolution kinetics test was performed.…”

Section: Discussionmentioning

confidence: 99%

Optimization of Delivery and Bioavailability of Encapsulated Caffeic Acid

Stanciauskaite,

Poskute,

Kurapkiene

et al. 2023

Foods

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Caffeic acid is a widely distributed phenolic acid. It is described in the scientific literature that caffeic acid has poor solubility. The aim of this study was to improve the solubility of caffeic acid for better dissolution kinetics when administered orally. During the study, oral capsules of different compositions were modeled. The results of the disintegration test revealed that the excipients affected the disintegration time of the capsules. The excipient hypromellose prolonged the disintegration time and dissolution time of caffeic acid. The dissolution kinetics of caffeic acid from capsules depend on the chosen excipients. P407 was more effective compared to other excipients and positively affected the dissolution kinetics of caffeic acid compared to other excipients. When the capsule contained 25 mg of β-cyclodextrin, 85% of the caffeic acid was released after 60 min. When the capsule contained 25–50 mg poloxamer 407, more than 85.0% of the caffeic acid was released from capsules after 30 min. The research results showed that in order to improve the dissolution kinetics of caffeic acid, one of the important steps is to improve its solubility.

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“…Self-emulsifying systems have been developed in last years to increase the oral bioavailability of antiviral [144,145], cardiovascular [146][147][148][149][150], anti-tumour [151][152][153][154][155][156][157][158], antiemetic [159] or immunosuppressive [160] drugs, as well as of peptides [161][162][163][164][165], vitamins [166], nutraceuticals and natural compounds, such as resveratrol, curcumin or bruceine [167][168][169][170][171][172][173].…”

Section: Self-nano and Microemulsifying Drug Delivery Systemsmentioning

confidence: 99%

Current approaches in lipid-based nanocarriers for oral drug delivery

Plaza-Oliver

Santander-Ortega

Lozano

2021

Drug Deliv. and Transl. Res.

102

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Graphical abstract Lipid-based nanocarriers have gained much interest as carriers of drugs with poor oral bioavailability because of their remarkable advantages like low toxicity, affordable scale-up manufacture, strong biocompatibility or high drug loading efficiency. The potential of these nanocarriers lies in their ability to improve the gastrointestinal stability, solubility and permeability of their cargo drugs. However, achieving efficient oral drug delivery through lipid-based nanocarriers is a challenging task, since they encounter multiple physicochemical barriers along the gastrointestinal tract, e.g. the gastric acidic content, the intestinal mucus layer or the enzymatic degradation, that they must surmount to reach their target. These limitations may be turned into opportunities through a rational design of lipid-based nanocarriers. For that purpose, this review focuses on the main challenges of the oral route indicating the strategies undertaken for lipid-based nanocarriers in order to overcome them. Understanding their shortcomings and identifying their strengths will determine the future clinical success of lipid-based nanocarriers.

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A Soluplus/Poloxamer 407-based self-nanoemulsifying drug delivery system for the weakly basic drug carvedilol to improve its bioavailability

Cited by 11 publications

References 42 publications

Synthesis and Evaluation of Thiol-Conjugated Poloxamer and Its Pharmaceutical Applications

Synthesis and Evaluation of Thiol-Conjugated Poloxamer and Its Pharmaceutical Applications

Optimization of Delivery and Bioavailability of Encapsulated Caffeic Acid

Current approaches in lipid-based nanocarriers for oral drug delivery

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