scholarly journals A Novel Self-Emulsifying Drug Delivery System (SEDDS) Based on VESIsorb® Formulation Technology Improving the Oral Bioavailability of Cannabidiol in Healthy Subjects

Molecules ◽  
2019 ◽  
Vol 24 (16) ◽  
pp. 2967 ◽  
Author(s):  
Katharina Knaub ◽  
Tina Sartorius ◽  
Tanita Dharsono ◽  
Roland Wacker ◽  
Manfred Wilhelm ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Bioavailability ◽  
Cannabis Sativa ◽  
Pharmacokinetic Profile ◽  
Pharmacokinetic Parameters ◽  
Reference Formulation ◽  
Double Blind ◽  
Study Objective

Cannabidiol (CBD), a phytocannabinoid compound of Cannabis sativa, shows limited oral bioavailability due to its lipophilicity and extensive first-pass metabolism. CBD is also known for its high intra- and inter-subject absorption variability in humans. To overcome these limitations a novel self-emulsifying drug delivery system (SEDDS) based on VESIsorb® formulation technology incorporating CBD, as Hemp-Extract, was developed (SEDDS-CBD). The study objective was to evaluate the pharmacokinetic profile of SEDDS-CBD in a randomized, double-blind, cross-over design in 16 healthy volunteers under fasted conditions. As reference formulation, the same Hemp-Extract diluted with medium-chain triglycerides (MCT-CBD) was used. CBD dose was standardized to 25 mg. Pharmacokinetic parameters were analyzed from individual concentration-time curves. Single oral administration of SEDDS-CBD led to a 4.4-fold higher Cmax and a 2.85-/1.70-fold higher AUC0–8h/AUC0–24h compared to the reference formulation. Tmax was substantially shorter for SEDDS-CBD (1.0 h) compared to MCT-CBD (3.0 h). Subgroup analysis demonstrated a higher bioavailability in women compared to men. This difference was seen for MCT-CBD while SEDDS-CBD mitigated this gender effect. Overall, SEDDS-CBD showed a significant improvement for all determined pharmacokinetic parameters: increased CBD plasma values (Cmax), favorably enhanced bioavailability (AUC) and fast absorption (Tmax). No safety concerns were noted following either administration.

scholarly journals Preparation and Characterization of a Novel Swellable and Floating Gastroretentive Drug Delivery System (sfGRDDS) for Enhanced Oral Bioavailability of Nilotinib

Pharmaceutics ◽  
2020 ◽  
Vol 12 (2) ◽  
pp. 137 ◽  
Author(s):  
Hong-Liang Lin ◽  
Ling-Chun Chen ◽  
Wen-Ting Cheng ◽  
Wei-Jie Cheng ◽  
Hsiu-O Ho ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Side Effects ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Bioavailability ◽  
Optimal Dose ◽  
Pharmacokinetic Profile ◽  
Medical Need ◽  
Tablet Hardness

Regarding compliance and minimization of side effects of nilotinib therapy, there is a medical need to have a gastroretentive drug delivery system (GRDDS) to enhance the oral bioavailability that is able to administer an optimal dose in a quaque die (QD) or daily manner. In this study, the influence on a swelling and floating (sf) GRDDS composed of a polymeric excipient (HPMC 90SH 100K, HEC 250HHX, or PEO 7000K) and Kollidon® SR was examined. Results demonstrated that PEO 7000K/Kollidon SR (P/K) at a 7/3 ratio was determined to be a basic GRDDS formulation with optimal swelling and floating abilities. MCC PH102 or HPCsssl,SFP was further added at a 50% content to this basic formulation to increase the tablet hardness and release all of the drug within 24 h. Also, the caplet form and capsule form containing the same formulation demonstrated higher hardness for the former and enhanced floating ability for the latter. A pharmacokinetic study on rabbits with pH values in stomach and intestine similar to human confirmed that the enhanced oral bioavailability ranged from 2.65–8.39-fold with respect to Tasigna, a commercially available form of nilotinib. In conclusion, the multiple of enhancement of the oral bioavailability of nilotinib with sfGRDDS could offer a pharmacokinetic profile with therapeutic effectiveness for the QD administration of a reasonable dose of nilotinib, thereby increasing compliance and minimizing side effects.

Improved antimicrobial activity and oral bioavailability of Delafloxacin by self-nanoemulsifying drug delivery system (SNEDDS)

2021 ◽  
pp. 102572
Author(s):  
Md. Khalid Anwer ◽  
Muzaffar Iqbal ◽  
Mohammed F. Aldawsari ◽  
Ahmed Alalaiwe ◽  
Muqtader Mohammad ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Antimicrobial Activity ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Bioavailability

scholarly journals Design and development of microemulsion drug delivery system of acyclovir for improvement of oral bioavailability

2006 ◽  
Vol 7 (3) ◽  
Author(s):  
Pradip Kumar Ghosh ◽  
Rita J. Majithiya ◽  
Manish L. Umrethia ◽  
Rayasa S. R. Murthy
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Bioavailability ◽  
Design And Development

Greatly enhanced oral bioavailability of propranolol using the HALOTM liver-bypass drug delivery system

1994 ◽  
pp. 306-309
Author(s):  
S.G. Barnwell ◽  
L. Gauci ◽  
R.J. Harris ◽  
D. Attwood ◽  
G. Littlewood ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Bioavailability

scholarly journals Improved Dissolution and Oral Bioavailability of Valsartan Using a Solidified Supersaturable Self-Microemulsifying Drug Delivery System Containing Gelucire® 44/14

Pharmaceutics ◽  
2019 ◽  
Vol 11 (2) ◽  
pp. 58 ◽  
Author(s):  
Dong Shin ◽  
Bo Chae ◽  
Yoon Goo ◽  
Ho Yoon ◽  
Chang Kim ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Bioavailability ◽  
Amorphous State ◽  
Poloxamer 407 ◽  
Enhanced Dissolution ◽  
Previous Formulation ◽  
Practical Development ◽  
Precipitation Inhibitor

To improve the dissolution and oral bioavailability of valsartan (VST), we previously formulated a supersaturable self-microemulsifying drug delivery system (SuSMED) composed of Capmul® MCM (oil), Tween® 80 (surfactant), Transcutol® P (cosurfactant), and Poloxamer 407 (precipitation inhibitor) but encountered a stability problem (Transcutol® P-induced weight loss in storage) after solidification. In the present study, replacing Transcutol® P with Gelucire® 44/14 resulted in a novel SuSMED formulation, wherein the total amount of surfactant/cosurfactant was less than that of the previous formulation. Solidified SuSMED (S-SuSMED) granules were prepared by blending VST-containing SuSMED with selective solid carriers, L-HPC and Florite® PS-10, wherein VST existed in an amorphous state. S-SuSMED tablets fabricated by direct compression with additional excipients were sufficiently stable in terms of drug content and impurity changes after 6 months of storage at accelerated conditions (40 ± 2 °C and 75 ± 5% relative humidity). Consequently, enhanced dissolution was obtained (pH 1.2, 2 h): 6-fold for S-SuSMED granules against raw VST; 2.3-fold for S-SuSMED tablets against Diovan® (reference tablet). S-SuSMED tablets increased oral bioavailability in rats (10 mg/kg VST dose): approximately 177–198% versus raw VST and Diovan®. Therefore, VST-loaded S-SuSMED formulations might be good candidates for practical development in the pharmaceutical industry.

Enhanced Oral Bioavailability and Improved Biological Activities of a Quercetin/Resveratrol Combination Using a Liquid Self-Microemulsifying Drug Delivery System

Planta Medica ◽  
2020 ◽  
Author(s):  
Patcharawalai Jaisamut ◽  
Subhaphorn Wanna ◽  
Surasak Limsuwan ◽  
Sasitorn Chusri ◽  
Kamonthip Wiwattanawongsa ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Bioavailability ◽  
Biological Activities ◽  
Area Under The Curve ◽  
Aqueous Solubility ◽  
The Self

AbstractBoth quercetin and resveratrol are promising plant-derived compounds with various well-described biological activities; however, they are categorized as having low aqueous solubility and labile natural compounds. The purpose of the present study was to propose a drug delivery system to enhance the oral bioavailability of combined quercetin and resveratrol. The suitable self-microemulsifying formulation containing quercetin together with resveratrol comprised 100 mg Capryol 90, 700 mg Cremophor EL, 200 mg Labrasol, 20 mg quercetin, and 20 mg resveratrol, which gave a particle size of 16.91 ± 0.08 nm and was stable under both intermediate and accelerated storage conditions for 12 months. The percentages of release for quercetin and resveratrol in the self-microemulsifying formulation were 75.88 ± 1.44 and 86.32 ± 2.32%, respectively, at 30 min. In rats, an in vivo pharmacokinetics study revealed that the area under the curve of the self-microemulsifying formulation containing quercetin and resveratrol increased approximately ninefold for quercetin and threefold for resveratrol compared with the unformulated compounds. Moreover, the self-microemulsifying formulation containing quercetin and resveratrol slightly enhanced the in vitro antioxidant and cytotoxic effects on AGS, Caco-2, and HT-29 cells. These findings demonstrate that the self-microemulsifying formulation containing quercetin and resveratrol could successfully enhance the oral bioavailability of the combination of quercetin and resveratrol without interfering with their biological activities. These results provide valuable information for more in-depth research into the utilization of combined quercetin and resveratrol.

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