Optimized piperine–phospholipid complex with enhanced bioavailability and hepatoprotective activity

Biswas, Sayan; Kar, Amit; Bannerjee, Subhadip; Charoensub, Rawiwan; Duangyod, Thidarat

doi:10.1080/10837450.2020.1835956

Cited by 23 publications

(17 citation statements)

References 45 publications

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“…Advanced, high-performing and standardized Cuscuta reflexa extract phospholipid complexes were used in this study to improve the efficacy and safety of the Cuscuta reflexa plant extract. Variations in extract/phospholipid (w/ w) ratios were used to incorporate the whole extract into phytosomes, and the Box Behnken Design was used to change the desirability function for 3-factors and 3-levels 20) . Independent variables (factors) were the amount of soya lecithin and Cuscuta reflexa extract (X1) , temperature (X2) and sonication time (X3) for two dependent variables i.e.…”

mentioning

confidence: 99%

Optimization and Characterization of <i>Cuscuta reflexa </i>Extract Loaded Phytosomes by the Box-Behnken Design to Improve the Oral Bioavailability

Alshahrani

2022

J. Oleo Sci.

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IntroductionRecent literature findings have shown bioactive compounds utilized in current therapies have natural origins for the vast majority of the time, according to recent literature studies. This means that they are obtained from natural items or their chemical structure was inspired by natural goods for the most part 1) . Cuscuta reflexa, a member of the Convolvulaceae family, is one such therapeutic plant. According to previous studies, the antioxidant, antibacterial, antispasmodic, hemodynamic, antihypertensive, antidiabetic, hepatoprotective properties of Cuscuta reflexa have been demonstrated 2−4) . Also, from this herb, a wide range of bioactive constituents have been isolated; among them are kaempferol, astragalin, myricetin, quercetin, and sesamin. Other bioactive constituents found in this herb include isorhamnetol, linoleic and/or oleic acids, stearic and/or palmitic acids, luteolin, and sesamin 5−8) .

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confidence: 99%

Optimization and Characterization of <i>Cuscuta reflexa </i>Extract Loaded Phytosomes by the Box-Behnken Design to Improve the Oral Bioavailability

Alshahrani

2022

J. Oleo Sci.

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“…) of piperine and-P=O of HSPC [30]. These results were supported by PXRD, which showed piperinephospholipid complexation by reduced piperine crystallinity and amorphous state formation [30].…”

Section: Lipid-based Drug Delivery Systemsmentioning

confidence: 61%

“…These results were supported by PXRD, which showed piperinephospholipid complexation by reduced piperine crystallinity and amorphous state formation [30]. The physical mixture did not show any significant change in pharmacokinetic parameters compared to pure piperine, indicating that complexation was a determinant in pharmacokinetic improvement [30].…”

Section: Lipid-based Drug Delivery Systemsmentioning

confidence: 84%

Recent Strategies for Improving Solubility and Oral Bioavailability of Piperine

2021

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Piperine, the main bioactive compound found in black pepper (Piper nigrum L.), has long been used in Ayurveda and traditional Chinese medicine (TCM). This compound has remarkable potential pharmacological properties, including being anti-inflammatory, antimicrobial, anticancer, anticonvulsant, antidepressant, neuroprotective, and hepatoprotective. Recent studies have reported piperine activity as an antiviral against SARS-CoV-2, which caused COVID-19. Nevertheless, the clinical use of piperine is still limited, due to its poor water solubility and bioavailability; therefore, various approaches have been developed in order to solve these limitations. This review summarises recent studies (i.e. uploaded to electronic databases in the last 10 y) regarding strategies that have been investigated to improve piperine’s solubility and pharmacokinetic properties, using ‘piperine’, ‘solubility’, ‘bioavailability’, and ‘formulation’ as keywords. Articles that have focused on piperine as the main compound were selected and sorted based on their modification and formulation types. Studies reported various approaches: from derivatives and analogue synthesis, crystal engineering, complexation, particle size reduction (micro-and nanonisation), and lipid-and polymer-based drug delivery systems, to inorganic and hybrid nanoparticles. This review also highlights limitations and challenges for these approaches and encourages further studies to optimise piperine’s potential benefits.

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“…The solubility of the complex in water and n- Octanol was improved by ~ 29.5-fold and ~ 3.2-fold, respectively, compared to pure PIP. Furthermore, the C max of the drug from complex (9.75 ± 2.17 μg/ml) was significantly improved compared to the C max of PIP from the pure drug (8 ± 0.21 μg/ml) [ 106 ]. These studies demonstrated phospholipid complexation’s ability to improve the drug’s bioavilability.…”

Section: Pharmacosome (Phc)mentioning

confidence: 99%

Drug complexes: Perspective from Academic Research and Pharmaceutical Market

et al. 2023

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Despite numerous research efforts, drug delivery through the oral route remains a major challenge to formulation scientists. The oral delivery of drugs poses a significant challenge because more than 40% of new chemical entities are practically insoluble in water. Low aqueous solubility is the main problem encountered during the formulation development of new actives and for generic development. A complexation approach has been widely investigated to address this issue, which subsequently improves the bioavailability of these drugs. This review discusses the various types of complexes such as metal complex (drug-metal ion), organic molecules (drug-caffeine or drug-hydrophilic polymer), inclusion complex (drug-cyclodextrin), and pharmacosomes (drug-phospholipids) that improves the aqueous solubility, dissolution, and permeability of the drug along with the numerous case studies reported in the literature. Besides improving solubility, drug-complexation provides versatile functions like improving stability, reducing the toxicity of drugs, increasing or decreasing the dissolution rate, and enhancing bioavailability and biodistribution. Apart, various methods to predict the stoichiometric ratio of reactants and the stability of the developed complex are discussed. Graphical Abstract

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Optimized piperine–phospholipid complex with enhanced bioavailability and hepatoprotective activity

Cited by 23 publications

References 45 publications

Optimization and Characterization of <i>Cuscuta reflexa </i>Extract Loaded Phytosomes by the Box-Behnken Design to Improve the Oral Bioavailability

Optimization and Characterization of <i>Cuscuta reflexa </i>Extract Loaded Phytosomes by the Box-Behnken Design to Improve the Oral Bioavailability

Recent Strategies for Improving Solubility and Oral Bioavailability of Piperine

Drug complexes: Perspective from Academic Research and Pharmaceutical Market

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