Preparation and Characterization of Mucoadhesive Nanoemulsion containing Piperine for Nasal Drug Delivery System

Author(s):  
Deepika Yadav ◽  
Avijit Mazumder ◽  
Roop K Khar

Piperine a bio active constituent isolated from pepper (Piper nigrum and Piper longum L.) is a naturally occurring alkaloid have validated for several health effects and valuable therapeutic effects. However, its biological applications are limited due to its poor aqueous solubility. This emphasizes on the development of new drug delivery system for piperine to improve its in-vivo bioavailability. The present study reports the development and characterization of mucoadhesive nanoemulsion (MNE) containing piperine. MNE formulations were prepared using titration method and characterized in relation to appearance, globule size, zeta potential, thermodynamic stability testing, Ex-vivo evaluation and in-vitro drug permeation study. The MNE of piperine have small globule size (˂ 150nm) and positive zata potential. The spherical surface was confirmed from TEM. pH of MNE was compatible with nasal administration. In vitro release of MNE system in nasal mucosal membrane demonstrated prompt and effective release with more than 75 % of drug release in 4 h.

Nanomaterials ◽  
2021 ◽  
Vol 11 (11) ◽  
pp. 2920
Author(s):  
Ameeduzzafar Zafar ◽  
Syed Sarim Imam ◽  
Nabil K. Alruwaili ◽  
Omar Awad Alsaidan ◽  
Mohammed H. Elkomy ◽  
...  

Hypertension is a cardiovascular disease that needs long-term medication. Oral delivery is the most common route for the administration of drugs. The present research is to develop piperine self-nanoemulsifying drug delivery system (PE-SNEDDS) using glyceryl monolinoleate (GML), poloxamer 188, and transcutol HP as oil, surfactant, and co-surfactant, respectively. The formulation was optimized by three-factor, three-level Box-Behnken design. PE-SNEDDs were characterized for globule size, emulsification time, stability, in-vitro release, and ex-vivo intestinal permeation study. The optimized PE-SNEDDS (OF3) showed the globule size of 70.34 ± 3.27 nm, percentage transmittance of 99.02 ± 2.02%, and emulsification time of 53 ± 2 s Finally, the formulation OF3 was transformed into solid PE-SNEDDS (S-PE-SNEDDS) using avicel PH-101 as adsorbent. The reconstituted SOF3 showed a globule size of 73.56 ± 3.54 nm, PDI of 0.35 ± 0.03, and zeta potential of −28.12 ± 2.54 mV. SEM image exhibited the PE-SNEDDS completely adsorbed on avicel. Thermal analysis showed the drug was solubilized in oil, surfactant, and co-surfactant. S-PE-SNEDDS formulation showed a more significant (p < 0.05) release (97.87 ± 4.89% in 1 h) than pure PE (27.87 ± 2.65% in 1 h). It also exhibited better antimicrobial activity against S. aureus and P. aeruginosa and antioxidant activity as compared to PE dispersion. The in vivo activity in rats exhibited better (p < 0.05) antihypertensive activity as well as 4.92-fold higher relative bioavailability than pure PE dispersion. Finally, from the results it can be concluded that S-PE-SNEDDS might be a better approach for the oral delivery to improve the absorption and therapeutic activity.


Author(s):  
Duaa J. Al-Tamimi ◽  
Ahmed A. Hussien

Abstract The present investigation aimed to formulate a liquid self-microemulsifying drug delivery system (SMEDDS) of tacrolimus to enhance its oral bioavailability by improving its dispersibility and dissolution rate. Four liquid SMEDDS were prepared using maisine CC as oil phase, labrasol ALF as surfactant and transcutol HP as co-surfactant based on the solubility studies of tacrolimus in these components. The phase behavior of the components and the area of microemulsion were evaluated using pseudoternary phase diagrams. The formulations were also assessed for thermodynamic stability, robustness to dilution, self-emulsification time, drug content, globule size and polydispersity index. The prepared SMEDDS formulations exhibited improved drug release compared to the pure drug powder. From this study, it was concluded that using a composition of 10% maisine CC, 67.5% labrasol ALF and 22.5% transcutol produced a liquid SMEDDS with good thermodynamic stability and enhanced in-vitro drug release profiles compared with pure tacrolimus powder. All which supports the use of self-micro emulsifying drug delivery systems as a promising approach to improve solubility, dissolution and stability of poorly soluble drugs like tacrolimus.


2009 ◽  
Vol 25 (2) ◽  
pp. 161-177 ◽  
Author(s):  
Bhavesh D. Kevadiya ◽  
Ghanshyam V. Joshi ◽  
Hasmukh A. Patel ◽  
Pravin G. Ingole ◽  
Haresh M. Mody ◽  
...  

Author(s):  
PAMU SANDHYA

Objective: The main objective of this study was to preparation and evaluation of efavirenz (EFV) to enhance its solubility and dissolution rate by self-emulsifying drug delivery system. Methods: EFV self-emulsifying drug delivery systems (SNEDDS) were formulated using different oils, surfactant, and co-surfactant. Peceol, Tween 20, and Capmul MCM were used as oil, surfactant, and co-surfactant, respectively, followed by the evaluation by the performance of different tests such as visual observation, solubility studies, thermodynamic stability study, transmittance studies, drug content, and in-vitro release study. Results: Fourier-transform infrared studies revealed negligible drug and polymer interaction. From the phase diagram, it was observed that self-emulsifying region was enhanced with increasing surfactant and co-surfactant concentrations with oil. F13 was selected as optimized formulation on the basis of physicochemical parameters, particle size, and in-vitro dissolution studies with the release of 98.39±5.10% drug in 1 hour. The optimized formulation size was found to be 156.7 nm as mean droplet size and Z-Average of 808.6 nm with -18.3 mV as zeta potential. Conclusion: The study demonstrated that SNEDDS was a promising strategy to enhance the dissolution rate of EFV by improving solubility.


2014 ◽  
Vol 62 (12) ◽  
pp. 1173-1179 ◽  
Author(s):  
Hongxing Ma ◽  
Mingjuan Chu ◽  
Kiyoshi Itagaki ◽  
Ping Xin ◽  
Xuegang Zhou ◽  
...  

2016 ◽  
Vol 105 (11) ◽  
pp. 3387-3398 ◽  
Author(s):  
Emelie Ahnfelt ◽  
Erik Sjögren ◽  
Per Hansson ◽  
Hans Lennernäs

Sign in / Sign up

Export Citation Format

Share Document