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.

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.

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
Sign in / Sign up

Export Citation Format

Share Document