Statistical Design of Sustained-Release Tablet Garcinia cambogia Extract and Bioconverted Mulberry Leaf Extract for Anti-Obesity

Lee, Hye-Jin; Na, Young-Guk; Han, Min-Gu; Pham, Thi Mai Anh; Lee, Hyeonmin; Lee, Hong-Ki; Myung, Chang‐Seon; Han, Joo‐Hui; Kang, Jong Seong; Kim, Kyung‐Tae; Cho, Cheong-Weon

doi:10.3390/pharmaceutics12100932

Cited by 6 publications

(3 citation statements)

References 24 publications

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“…Network pharmacology is an emerging discipline that is based on the statistical analysis of data, virtual computing and the observation of component-target-disease-pathway interactions retrieved from network databases (23). MLE have been previously demonstrated to alleviate hyperglycemia, hyperlipidemia, obesity, oxidation and inflammation (24)(25)(26)(27)(28). Pharmacological analysis has indicated that the active components in MLE include β-carotene, quercetin, β-sitosterol, kaempferol and arachidonic acid, all of which can exert beneficial effects against obesity (29)(30)(31)(32)(33).…”

Section: Discussionmentioning

confidence: 99%

Network pharmacology approach to evaluate the therapeutic effects of mulberry leaf components for obesity

Wang¹,

Dong²

2021

Exp Ther Med

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Obesity is a chronic condition that has become a serious public health challenge globally due to the association with a high incidence of complications. Mulberry leaf is one of the most commonly used medicinal and herbal medicines that has been reported to ameliorate obesity and hyperlipidemia. However, the mechanism remains unclear. In the present study, a network pharmacology approach was used to explore the potential mechanism underlying the effects of mulberry leaf extract on obesity. First, the potential targets of mulberry leaf and obesity were predicted using SwissTargetPrediction, Online Mendelian Inheritance in Man, GeneCards and Comparative Toxicogenomics Database databases, which were then used to construct the protein-protein interaction networks. Gene ontology (GO) enrichment and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analyzes were performed using R version 3.6.3. Finally, results of this network analysis were verified by using the mulberry leaf extract to treat high-fat diet-induced obese mice. In total, 24 target genes associated with obesity that could potentially be affected by mulberry leaf treatment were predicted by network pharmacology, using which top seven related pathways were determined by KEGG enrichment analysis. Triglyceride (TG) and total cholesterol (TC) levels in mice serum were detected using TG and TC assay kits. Hepatic fat accumulation was detected by H&E staining whereas liver lipid droplets were detected by Oil red O staining in mice tissues. The expression of IL-1β, NF-κB inhibitor α, inducible nitric oxide synthase, AMP-activated protein kinase (AMPK), sterol regulatory element-binding proteins and fatty acid synthase in the visceral white adipose tissues of mice was analyzed by western blotting. The expression of TNF-α, peroxisome proliferator activated receptor (PPAR)D, PPARG, fatty acid amide hydrolase (FAAH) and hydroxysteroid 11-β dehydrogenase 1 (HSD11B1) in the visceral white adipose tissues of mice was detected by reverse transcription-quantitative PCR. Mulberry leaf extract was found to reduce fat accumulation and hepatic lipid droplet formation. Mulberry leaf also alleviated inflammation and lipogenesis whilst promoting lipid catabolism and fatty acid oxidation by promoting the AMPK signaling pathway. The possible anti-obesity effects of mulberry leaf on the mice may be due to the downregulation of TNF-α, PPARD and PPARG and the upregulation of FAAH and HSD11B1. These results were consistent with the GO enrichment analysis and suggested that mulberry leaf may regulate lipid metabolism and catabolism, fatty acid metabolism and biosynthesis and the inflammatory response to reduce obesity.

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Section: Discussionmentioning

confidence: 99%

Network pharmacology approach to evaluate the therapeutic effects of mulberry leaf components for obesity

Wang¹,

Dong²

2021

Exp Ther Med

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“…Additionally, G. cambogia and G. indica were found to contain the highest (−)-HCA and its lactone levels, and suggestive that G. indica can be used instead of G. cambogia especially if targeting its HCA. Likewise, (−)hydroxycitric acid was analyzed in G. cambogia commercial samples using HPLC/UV. , The mean recovery of HCA from G. cambogia extracts ranged 98.4–100.5% with coefficients of variation of 0.25–0.63% and accuracy range of 2–10 μg, reflecting that the method is validated for the routine analysis of HCA in commercial G. cambogia extracts . The method also offered selectivity compared to traditional acid base titration methods which quantify for total acids, not only targeting HCA .…”

Section: Introductionmentioning

confidence: 95%

Recent Advances in Garcinia cambogia Nutraceuticals in Relation to Its Hydroxy Citric Acid Level. A Comprehensive Review of Its Bioactive Production, Formulation, and Analysis with Future Perspectives

2022

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Garcinia cambogia (Gaertn.) Desr. (known as Malabar tamarind) is a popular traditional herbal medicine and is one of the well-known folk medicines reported for the treatment of obesity and incorporated in several nutraceuticals worldwide. These effects are mediated by a myriad of bioactive compounds with most effects attributed to its hydroxy citric acid (HCA) content. This review aims to present a holistic overview on novel trends in the production of G . cambogia bioactive components and how extraction optimization is important to ensure best product quality with its reported nanoformulations with particular emphasis on HCA content. Further, an overview of the different analytical approaches used for quality control assessment of G . cambogia plant and its nutraceuticals is presented highlighting both advantages and limitations. Moreover, analytical approaches for detecting G . cambogia metabolites in biological fluids with emphasis on HCA level to determine its pharmacokinetics and proof of efficacy are presented for the first time.

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“…The use of different types of polymers to control the drug release process represents one of the main aspects of the development of different types of matrix systems. Hydrophilic matrices are often the first choice in the development of modified-release pharmaceutical forms [10][11][12]. They are usually monolithic systems containing one or more hydrophilic polymers [13].…”

Section: Introductionmentioning

confidence: 99%

Polymer Tablet Matrix Systems for the Controlled Release of Dry Betula pendula Leaf Extract

Penkov,

Lukova,

Manev

et al. 2023

Polymers

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The aim of the study was to develop polymer matrix tablets with modified release of dry Betula pendula leaf extract and to investigate basic parameters influencing the drug release pattern. To fully assess the statistical significance of the influence of the individual factors in the tablet formulation development as well as the combination of them, Tukey’s tests and a complete 33 factor analysis of variance (ANOVA) were applied. The following three factors were studied at three levels (low, medium and high): influence of the hydrophobic/hydrophilic polymer ratio Ethylcellulose (EC)/Hydroxypropyl methylcellulose (HPMC) (40/60, 25/75 and 10/90), influence of HPMC molecular weight (500 kDa, 750 kDa and 1150 kDa), and influence of the compression force applied (1 t, 1.5 t and 2 t). The effect of these varied parameters on the drug release parameter t80 was evaluated statistically. Twenty-seven tablet models were formulated, including all possible combinations of the variables. The obtained drug release profiles demonstrated that a 25/75 (EC/HPMC) ratio was the most suitable for prolonging the release process. Increasing the molecular weight of HMPC from 500 kDa to 750–1150 kDa and applying higher compression force significantly influenced the studied t80 values and caused sustained drug release (t80 up to 7.97 h). The combination of the hydrophilic HPMC polymer with the hydrophobic EC can result in the formation of a promising drug-carrying matrix, offering effective control of the drug release process.

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Statistical Design of Sustained-Release Tablet Garcinia cambogia Extract and Bioconverted Mulberry Leaf Extract for Anti-Obesity

Cited by 6 publications

References 24 publications

Network pharmacology approach to evaluate the therapeutic effects of mulberry leaf components for obesity

Network pharmacology approach to evaluate the therapeutic effects of mulberry leaf components for obesity

Recent Advances in Garcinia cambogia Nutraceuticals in Relation to Its Hydroxy Citric Acid Level. A Comprehensive Review of Its Bioactive Production, Formulation, and Analysis with Future Perspectives

Polymer Tablet Matrix Systems for the Controlled Release of Dry Betula pendula Leaf Extract

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