scholarly journals Fabrication of Alginate-Based O/W Nanoemulsions for Transdermal Drug Delivery of Lidocaine: Influence of the Oil Phase and Surfactant

Molecules ◽  
2021 ◽  
Vol 26 (9) ◽  
pp. 2556
Author(s):  
Omar Sarheed ◽  
Manar Dibi ◽  
Kanteti V. R. N. S. Ramesh ◽  
Markus Drechsler

Transdermal drug delivery of lidocaine is a good choice for local anesthetic delivery. Microemulsions have shown great effectiveness for the transdermal transport of lidocaine. Oil-in-water nanoemulsions are particularly suitable for encapsulation of lipophilic molecules because of their ability to form stable and transparent delivery systems with good skin permeation. However, fabrication of nanoemulsions containing lidocaine to provide an extended local anesthetic effect is challenging. Hence, the aim of this study was to address this issue by employing alginate-based o/w nanocarriers using nanoemulsion template that is prepared by combined approaches of ultrasound and phase inversion temperature (PIT). In this study, the influence of system composition such as oil type, oil and surfactant concentration on the particle size, in vitro release and skin permeation of lidocaine nanoemulsions was investigated. Structural characterization of lidocaine nanoemulsions as a function of water dilution was done using DSC. Nanoemulsions with small droplet diameters (d < 150 nm) were obtained as demonstrated by dynamic light scattering (DLS) and cryo-TEM. These nanoemulsions were also able to release 90% of their content within 24-h through PDMS and pig skin and able to the drug release over a 48-h. This extended-release profile is highly favorable in transdermal drug delivery and shows the great potential of this nanoemulsion as delivery system.

2019 ◽  
Vol 11 (1) ◽  
pp. 55
Author(s):  
Shikha Baghel Chauhan ◽  
Tanveer Naved ◽  
Nayyar Parvez

Objective: The combination therapy of ethinylestradiol and testosterone in post-menopausal females has shown improved sexual response and libido. The present studies were designed to develop a suitable matrix-type transdermal drug delivery system (TDDS) of ethinylestradiol and testosterone using the polymer chitosan.Methods: Five formulations (ET1 to ET5) were developed by varying the concentration of polymer and keeping the drug load constant. Physical parameters and drug excipient interaction studies were evaluated in all the formulations. In vitro skin permeation profiles of ethinylestradiol and testosterone from various formulations were simultaneously characterized in a thermostatically controlled modified Franz Diffusion cell using HPLC. Based on the physical parameters and in vitro skin permeation profile formulation ET3 containing 30 mg/ml of chitosan was found to be the best and chosen for further studies. Optimized formulation was subjected to in vivo pharmacokinetic analysis in rats using ELISA.Results: Stability profile of patch formulation ET3 depicted stability up to 3 mo. One week skin irritation evaluation in rats indicated that formulation ET3 was nonirritating. Combination transdermal patch across rat skin showed a maximum release of 92.936 and 95.03 % in 60 h with a flux of 2.088 and 21.398 µg/cm2h for ethinylestradiol and testosterone respectively.Conclusion: The net result of this study is the formulation of a stable, non-irritating transdermal patch of ethinylestradiol and testosterone, with good bioavailability and can be used as Estrogen Replacement Therapy (ERT) in postmenopausal women.


Polymers ◽  
2021 ◽  
Vol 13 (19) ◽  
pp. 3345
Author(s):  
Taif Ali Khan ◽  
Abul Kalam Azad ◽  
Shivkanya Fuloria ◽  
Asif Nawaz ◽  
Vetriselvan Subramaniyan ◽  
...  

The purpose of the present study was to develop emulsions encapsulated by chitosan on the outer surface of a nano droplet containing 5-fluorouracil (5-FU) as a model drug. The emulsions were characterized in terms of size, pH and viscosity and were evaluated for their physicochemical properties such as drug release and skin permeation in vitro. The emulsions containing tween 80 (T80), sodium lauryl sulfate, span 20, and a combination of polyethylene glycol (PEG) and T20 exhibited a release of 88%, 86%, 90% and 92%, respectively. Chitosan-modified emulsions considerably controlled the release of 5-FU compared to a 5-FU solution (p < 0.05). All the formulations enabled transportation of 5-FU through a rat’s skin. The combination (T80, PEG) formulation showed a good penetration profile. Different surfactants showed variable degrees of skin drug retention. The ATR-FTIR spectrograms revealed that the emulsions mainly affected the fluidization of lipids and proteins of the stratum corneum (SC) that lead to enhanced drug permeation and retention across the skin. The present study concludes that the emulsions containing a combination of surfactants (Tween) and a co-surfactant (PEG) exhibited the best penetration profile, prevented the premature release of drugs from the nano droplet, enhanced the permeation and the retention of the drug across the skin and had great potential for transdermal drug delivery. Therefore, chitosan-coated 5-FU emulsions represent an excellent possibility to deliver a model drug as a transdermal delivery system.


Author(s):  
SADIA ANWAR ◽  
SYED UMER JAN ◽  
RAHMAN GUL

Objective: The purpose of this study was to formulate and evaluate of Celecoxib cream and it’s in vitro release study. Methods: The release study was conducted, using dialysis cellulose membrane, in Franz cells. The donor chamber was filled with phosphate buffer pH 7.4, released medium were analyzed by UV-Vis spectrophotometer at 250 nm. Kinetics model was used for calculations. The cream was followed by different evaluations like pH measurement, homogeneity, spreadability, stability study, drug content, SEM, XRD studies and skin irritation test was used for the reliability of physical conditions and chemical relation. DD solver and SPSS were used for statistical analyzation of the data. Results: The best in vitro drug release profile achieved with thyme oil in Celecoxib cream. Formulation F2 showed the highest (83%) released. The results of the Celecoxib (1%) were suitable in all constraints. The prepared Celecoxib cream was encouraging for the formulation of transdermal drug delivery. Conclusion: The Celecoxib cream was successfully prepared and could be beneficial for transdermal drug delivery.


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.


Author(s):  
Muhammad Wahab Amjad ◽  
Maria Abdul Ghafoor Raja

The purpose of this study was to develop liposome-enriched Ketoprofen liposomal hydrogels and carry out in vitro release profile experiment. The aim was to achieve sustained topical drug delivery for extended time interval from liposomal gels. Phosphatidylcholine, Cholesterol and Ketoprofen were dissolved in chloroform/methanol (2:1, v/v) mixture and subsequently transferred to a flask attached to rotavapor. The liposomes were assessed for particle size and percent drug entrapment. F-7 and F-8 batches were found to be optimized batches having optimum sizes, drug entrapment efficiencies and cumulative drug releases. F-8 batch was further evaluated for stability. The results show that the prepared liposomes of Ketoprofen might turn out to be potential candidates for effective and safe sustained drug delivery thereby resulting in the reduction of dosing frequency.


2021 ◽  
Vol 7 (2) ◽  
pp. 519-522
Author(s):  
Natalia Rekowska ◽  
Alexander Riess ◽  
Robert Mau ◽  
Thomas Eickner ◽  
Hermann Seitz ◽  
...  

Abstract Drug delivery systems (DDS) are suitable for controlled local drug release in order to ensure safety and effectiveness of medical treatment. The choice and characterization of biomaterials that can be used as a DDS is a challenging step in the administration of drugs. Novel 3D printing photopolymerization-based techniques create the possibility for designing individual, patient-tailored DDS. Poly(ethylene glycol) diacrylate`s (PEGDA`s) chemical and biological properties make it a suitable photopolymerisable resin for the creation of DDS. This study describes the in vitro release of the antiseptic drug chlorhexidine (CHX) from UV-cured PEGDA and its copolymers (butanediol diacrylate, pentaerythritol triacrylate and pentaerythritol tetraacrylate) samples. A substantial decrease in CHX release with increasing concentration of the copolymers in comparison to pure PEGDA was obtained only for butanediol diacrylate. For pentaerythritol triacrylate and pentaerythritol tetraacrylate only a tendency of decreased CHX release with increasing concentration was detected. Therefore, release profiles of the low molecular drug CHX from PEGDA samples could be modified by the addition of copolymers with a different number of acrylate groups and PEGDA can be considered as a promising candidate for the preparation of novel DDS.


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