A three-pronged formulation approach to improve oral bioavailability and therapeutic efficacy of two lipophilic drugs with gastric lability

Jyoti, Jivan; Anandhakrishnan, Nandha Kumar; Singh, Sachin Kumar; Kumar, Bimlesh; Gulati, Monica; Kuppusamy, Gowthamarajan; Kumar, Rajesh; Yadav, Ankit; Kapoor, Bhupinder; Pandey, Narendra Kumar; Som, Sananda; Mohanta, Souvik; Melkani, Indu; Khursheed, Rubiya; Narang, Rakesh

doi:10.1007/s13346-019-00635-0

Cited by 19 publications

(5 citation statements)

References 21 publications

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“…However, its poor bioavailability has been a major challenge in realizing its full therapeutic potential. Studies over the past three decades have shown that curcumin has limited absorption, rapid metabolism, and a short half-life, which severely restricts its bioavailability [7,9,13,14] .…”

Section: Pharmaceutical Challenges Of Curcuminmentioning

confidence: 99%

Chemopreventive approach of Indian spice “Curcumin” in the treatment of breast cancer

Deb,

Mishra,

Kumar

et al. 2023

Trends Immunother.

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One of the primary concerns for women in good health is breast cancer. The most typical hazardous growth is this one. It spreads easily, and the clinical conditions are terrible. Bosom illness is the second‐most common type of malignant tumor that regularly causes women to pass away in the U.S. bosom malignant growth is the most well‐known disease among women worldwide, with 2.1 million cases reported in 2018 and more than 620,000 fatalities per year. Natural components are viewed as promising alternatives for the development of novel anti‐tumor drugs. Curcumin, also termed diferuloylmethane, is a yellow pigment made by the turmeric plant, Curcuma longa Linn. It is the curcuminoid and polyphenol present in the plant’s root that is most abundant. The antioxidant and anti‐inflammatory qualities of curcumin have been demonstrated, and it is frequently utilized in traditional medicine and cuisine. Due to its sophisticated pharmacological capabilities of chemoprevention and anticancer effects, curcumin, the main component of turmeric, has been linked to the treatment of breast cancer. The morbidity or mortality of the disease have not been significantly decreased by current breast cancer treatment options such as surgery, radiation, adjuvant chemotherapy, or hormone therapy. The expansion, estrogen receptor (trauma center), and human epidermal development factor receptor 2 (HER2) pathways are all involved in the activity of curcumin in illness. In breast cancer cells, curcumin is also known to regulate microRNA, cell stage-related characteristics, and apoptosis. This study reviews recent research on the atomic targets and anticancer effects of curcumin in breast cancer.

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Section: Pharmaceutical Challenges Of Curcuminmentioning

confidence: 99%

Chemopreventive approach of Indian spice “Curcumin” in the treatment of breast cancer

Deb,

Mishra,

Kumar

et al. 2023

Trends Immunother.

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“…In recent years, improved bioavailability of poorly soluble drugs formulated as LS systems was reported in a number of in vivo studies (47)(48)(49)(50)(51)(52)(53), including the studies performed in healthy human volunteers (27,54). Jhaveri et al (50), for example, conducted a study with carvedilol as a model drug.…”

Section: Drug Dissolution Enhancementmentioning

confidence: 99%

Liquisolid systems as a novel approach in formulation and manufacturing of solid dosage forms: Challenges and perspectives

Aleksić¹,

Glišić²,

Parojčić³

2022

Arhiv za farmaciju

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Liquisolid systems are a novel, promising platform for the production of solid dosage forms with a high liquid content, i.e. dispersion of the drug in a suitable, hydrophilic, non-volatile liquid vehicle or liquid drug. This technology requires conventional, but highly porous excipients (carrier and coating material in the appropriate ratio) able to absorb/adsorb liquid medication, resulting in both good flowability and acceptable compression properties. This approach has shown great potential to improve the dissolution rate and bioavailability of poorly soluble drugs, and has been recognized as a good alternative to common, more complex and expensive techniques. A variety of applications of this simple technique have been investigated recently, including the preparation of: modified release tablets, orally disintegrating tablets, solid dosage forms with liquid herbal extracts, etc. This emerging technology has numerous advantages, and the most important are: simplicity, cost-effectiveness, applicability in large scale production and environmental friendliness. However, it is accompanied by certain challenges as well, such as limited applicability in the case of highly dosed drugs. This article aims to give a comprehensive overview of recent progress regarding the potential applications of this technology, as well as to give an insight into the new liquisolid-based techniques intending to further support its commercial applicability.

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“…In a multitude of in vitro studies, including a wide variety of model drugs, significantly improved dissolution profiles were achieved with LS tablets compared to directly compressed tablets of the same composition or similar commercially available formulations [ 7 , 8 , 9 , 10 , 11 , 12 ]. The results of in vivo studies indicate an improvement in the rate and extent of absorption, higher plasma concentrations, improved bioavailability, and significantly more pronounced therapeutic effects [ 13 , 14 , 15 , 16 , 17 , 18 , 19 ]. However, despite its advantages, the LS technology has yet to find its place in practice.…”

Section: Introductionmentioning

confidence: 99%

Application of Machine-Learning Algorithms for Better Understanding the Properties of Liquisolid Systems Prepared with Three Mesoporous Silica Based Carriers

et al. 2023

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The processing of liquisolid systems (LSS), which are considered a promising approach to improving the oral bioavailability of poorly soluble drugs, has proven challenging due to the relatively high amount of liquid phase incorporated within them. The objective of this study was to apply machine-learning tools to better understand the effects of formulation factors and/or tableting process parameters on the flowability and compaction properties of LSS with silica-based mesoporous excipients as carriers. In addition, the results of the flowability testing and dynamic compaction analysis of liquisolid admixtures were used to build data sets and develop predictive multivariate models. In the regression analysis, six different algorithms were used to model the relationship between tensile strength (TS), the target variable, and eight other input variables. The AdaBoost algorithm provided the best-fit model for predicting TS (coefficient of determination = 0.94), with ejection stress (ES), compaction pressure, and carrier type being the parameters that influenced its performance the most. The same algorithm was best for classification (precision = 0.90), depending on the type of carrier used, with detachment stress, ES, and TS as variables affecting the performance of the model. Furthermore, the formulations with Neusilin® US2 were able to maintain good flowability and satisfactory values of TS despite having a higher liquid load compared to the other two carriers.

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A three-pronged formulation approach to improve oral bioavailability and therapeutic efficacy of two lipophilic drugs with gastric lability

Cited by 19 publications

References 21 publications

Chemopreventive approach of Indian spice “Curcumin” in the treatment of breast cancer

Chemopreventive approach of Indian spice “Curcumin” in the treatment of breast cancer

Liquisolid systems as a novel approach in formulation and manufacturing of solid dosage forms: Challenges and perspectives

Application of Machine-Learning Algorithms for Better Understanding the Properties of Liquisolid Systems Prepared with Three Mesoporous Silica Based Carriers

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