Formulation Development and Bioavailability Evaluation of a Self-Nanoemulsified Drug Delivery System of Oleanolic Acid

Xi, Jia; Chang, Qi; Chan, Chak Keung; Meng, Zhao Yu; Wang, Geng Nan; Sun, Jia; Wang, Yi Tao; Tong, Henry H.Y.; Zheng, Ying

doi:10.1208/s12249-009-9190-9

Cited by 167 publications

(95 citation statements)

References 26 publications

(31 reference statements)

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Efforts have been made to improve their water solubility with chemically modified derivatives [7]. The synthesis of a non-covalent complex with hydrophilic cyclodextrins, as well as the use of nanosuspensions, enhancing both, solubility and stability (lipid emulsion containing corn oil or applying a self-nano-emulsified drug delivery system), are of special interest [9,92,93].…”

Section: Cellular Targets and Functions Affected By Oa Ua And Their mentioning

confidence: 99%

Antibacterial activity of oleanolic and ursolic acids and their derivatives

et al. 2010

View full text Add to dashboard Cite

Bacterial resistance to antibiotics is increasing at an alarming rate and many commonly used antibiotics are no longer effective.Thus, there is considerable interest in investigating novel antibacterial compounds, such as the plant-derived pentacyclic triterpenoids, including oleanolic acid (OA), ursolic acid (UA) and their derivatives. These compounds can be isolated from many medicinal and crop plants and their antibacterial, antiviral, antiulcer and anti-inflammatory effects are well documented. OA and UA are active against many bacterial species, particularly Gram-positive species, including mycobacteria. They inhibit bacterial growth and survival, and the spectrum of minimal inhibitory concentration (MIC) values is very broad. In addition, OA, UA and their derivatives display potent antimutagenic activity. Studies to identify the cellular targets and molecular mechanisms of OA and UA action were initiated a few years ago and it has already been demonstrated that both acids influence bacterial gene expression, the formation and maintenance of biofilms, cell autolysis and peptidoglycan turnover. Before these compounds can be used clinically as antimicrobial agents, further extensive studies are required to determine their cytotoxicity and the optimum mode of their application.

show abstract

Section: Cellular Targets and Functions Affected By Oa Ua And Their mentioning

confidence: 99%

Antibacterial activity of oleanolic and ursolic acids and their derivatives

et al. 2010

View full text Add to dashboard Cite

show abstract

“…Therefore, the SEDDS has an advantage in possessing a high solubilization capacity which ensures a higher dissolution rate in comparison to crude powder. 24) In addition, the drug dissolution profiles of the liquid SEDDS showed no significant differences when compared to those of the solid SEDDS (data not shown), suggesting that the SEDDS preserves a similar performance in emulsification regardless of the form (i.e. liquid or solid).…”

Section: Resultsmentioning

confidence: 91%

Enhanced Oral Bioavailability of Curcumin via a Solid Lipid-Based Self-Emulsifying Drug Delivery System Using a Spray-Drying Technique

Yan

Kim

Kwak

et al. 2011

Biological & Pharmaceutical Bulletin

View full text Add to dashboard Cite

In this study, a novel liquid self-emulsifying drug delivery system (SEDDS) containing curcumin was formulated and further developed into a solid form by a spray drying method using Aerosil 200 as the solid carrier. The optimum liquid SEDDS consisted of Lauroglycol Fcc, Labrasol and Transcutol HP as the oil phase, the surfactant and the co-surfactant at a weight ratio of 15.0 : 70.8 : 14.2 (w/w/w), respectively. There was no difference in droplet size between the emulsions obtained from the liquid and solid forms of SEDDS. Solid state characterization of the solid SEDDS was performed by scanning electron micrograph (SEM), differential scanning calorimetry (DSC), and X-ray powder diffraction (XRPD). The drug formulated in the solid SEDDS was quickly and completely dissolved within 5 min, both in 0.1 N HCl and phosphate buffer pH 6.8 dissolution media, whereas crude curcumin powder was significantly less dissoluble. The solid SEDDS formulation was stable for at least 3 months at 40°C with 75% relative humidity. After oral administration to rats, curcumin in the solid SEDDS resulted in significant improvement in in vivo absorption compared with that of curcumin powder. As the dose of curcumin formulated in solid SEDDS increased from 25 to 100 mg/kg, the C max and area under the drug concentration time curve (AUC) of curcumin were increased by 4.6 and 7.6 times, respectively. However, the over-proportional increase in the AUC in the higher dose group might be due to underestimation of AUC in the lower dose group. In conclusion, this solid SEDDS is a promising solid dosage form for poorly water-soluble curcumin.

show abstract

“…Lupane class comprises betulin, betulinic acid, lupeol [6,45]. Triterpenes are used as traditional herbal medicine and the esters of betulin and fatty acids are used in the production of cosmetics and as plasticizers for PVC [31,46] (Table 2). …”

Section: Occurrence Of Betulin In Naturementioning

confidence: 99%

Betulin, a Pentacyclic Tri-Terpenoid: An Hour to Rethink the Compound

Singh¹

2017

OAJTMR

View full text Add to dashboard Cite

Betulin, a pentacyclic triterpenoid member of lupane family occurs widely in numerous plants. Betulin, unlike most other constituents is easily isolated that it can be utilized for various pharmacological actions. It is interesting to know that betulin can be easily extracted from bark, stem, leaves, flower, roots etc. of the plant. This review summarizes plethora of reliable pharmacological activities like antiinflammatory, anti-ulcer, anti-diabetic, anti-bacterial, anti-microbial, anti-malarial, anti-viral, anti hyperlipidaemic, anti-cancer and anti HIV exhibited by betulin and its derivatives. For this it can be utilized in herbal as well as synthetic pharmaceutical industries because of its promising efficacy and low levels of toxicity. Although betulin possess a wide range of pharmacological activities, there is still lack of awareness of its proper utilization in the field of medicine. So, need of the hour is to refocus on naturally occurring betulin and its derivatives to avoid side effects caused by synthetic compounds utilized in treating various ailments. Therefore, the aim of the present review is to re-explore the potential of betulin, as an alternative to the compounds possessing higher side effects. Keywords: Table1:Represents the physical properties of betulin [1,30,31] Occurrence of Betulin in NatureBetulin has long been explored by research scientist because of the fact that it has anticancer properties [35,36] and its derivative Betulinic acid is favored due to its anti-HIV activity [12,6,37]. As mentioned in Figure 1: betulin has three most prominent positions where chemical modifications can be easily accomplished, namely primary hydroxyl group at position C-28, secondary hydroxyl group at position C-3, and alkene moiety at position C-20.The bio-chemical modifications at positions C-28 of the parent structure of betulin produces betulinic acid [12,27,[38][39][40][41]. The chief source of Betulin is bark of Birch trees, belonging to family Betulaceae the family of flowering plants. Mostly placed in order Fagales, it can also be placed in order Betulales. The subfamilies include Betuloideae genera Betula (birch), Alnus (alder) and Coryloideaegenera Carpinus (hornbeam), Corylus (hazel), Ostrya and Ostryopsis [42][43][44]. Betulin, a pentacyclictriterpenoid is derived from linear hydrocarbon squalene [31]. Triterpenes have three main classes oleane, ursane and lupane triterpenes. Lupane class comprises betulin, betulinic acid, lupeol [6,45]. Triterpenes are used as traditional herbal medicine and the esters of betulin and fatty acids are used in the production of cosmetics and as plasticizers for PVC [31,46] (Table 2). Pharmacological StudiesBetulin, as we all known till now possess vast pharmacological properties including choleritic, antihelmintic, powerful prophylactic, anti-HIV, antimutagene agent, antiviral, antifungal, anti-leukemia, anti-leishmanial, anti-inflammatory, immunomodulator activities. The latest research suggests some of the major pharmacological properties as discu...

show abstract

Formulation Development and Bioavailability Evaluation of a Self-Nanoemulsified Drug Delivery System of Oleanolic Acid

Cited by 167 publications

References 26 publications

Antibacterial activity of oleanolic and ursolic acids and their derivatives

Antibacterial activity of oleanolic and ursolic acids and their derivatives

Enhanced Oral Bioavailability of Curcumin via a Solid Lipid-Based Self-Emulsifying Drug Delivery System Using a Spray-Drying Technique

Betulin, a Pentacyclic Tri-Terpenoid: An Hour to Rethink the Compound

Contact Info

Product

Resources

About