ETHOSOMAL GEL PDF

Objective: The aim of the current investigation is to formulate and optimize a topical BDH ethosomal gel for weight gain control. The morphology and zeta potential of the optimized formulation were evaluated. Results: The size and entrapment efficiency percent had a direct positive relationship with the concentration of PC and negative relationship with ethanol and PG. Regression modeling indicated a good correlation between dependent and independent variables, where F16 was chosen as the optimized formulation.

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Ethosomes could enhance cell membrane fluidity and reduce epidermal membrane density to make macromolecular drugs through the stratum corneum into the deeper layers of the skin easily.

Methods: We used the orthogonal method to optimize the formulation of the ethosome preparation prepared by the ethonal infusion method. Ethosomal gels were characterized by using different analytical methods. Transdermal release rate in vitro have been demonstrated in Franz diffusion cells and the efficacy of drug-loaded nanocarriers in vivo was investigated in a mouse model. Compared with the free drug group, the ethosome preparation not only promotes the percutaneous absorption process of the macromolecular protein drugs but also shortened wound recovery time.

Conclusion: Hence, we provide a possible good design for ethosomal gel system that can load macromolecular protein peptide drugs to achieve transdermal drug administration, promoting the percutaneous absorption of the drug and improving the effect.

It is easily soluble in water and has a large molecular weight. Its molecular weight is Da and isoelectric point is 5. However, as a protein peptide drug, the molecular structure is easily destroyed in the gastrointestinal tract via oral administration and they have poor medication compliance.

The transdermal drug delivery system TDDS can make drugs directly exert the local effect and avoid the hepatic first-pass effect and gastrointestinal tract damage to maintain a constant blood concentration. Additionally, medication compliance in patients can significantly improve. As the outermost barrier of the skin, the stratum corneum is tightly connected and is the main obstacle and rate-limiting step for drug penetration into the skin.

However, these physicochemical methods also have potential disadvantages such as poor stability, a complicated preparation process and severe skin irritation. Traditional liposomes, due to their limited penetrating ability, cannot penetrate the stratum corneum and can only take drugs to the surface of the skin, failing to achieve the effect of deep treatment.

Additionally, the unique advantages of nontoxic and non-irritating ethosomes make them a research focus of TDDS. The efficacy of drug-loaded nanocarriers was tested by the transdermal release rate in vitro and in vivo pharmacokinetic study.

The purpose of this study is to develop ethosome gel system that can load macromolecular protein peptide drugs to achieve transdermal drug administration, significantly promoting the percutaneous absorption of the drug and improving the effect. Nanjing, China. San Francisco, USA. Sodium deoxycholate and phosphotungstic acid were obtained from Beijing Wokai Biological Technology Co.

Beijing, China. Carbomer was acquired from Dalian Meilun Biotechnology Co. Dalian, China. The experimental water was made using a Milli-Q ultrapure water system Millipore, Ireland. The acetonitrile and triethanolamine used were chromatographic grade, and other reagents were of analytical grade.

Jinan, China. All the animals were kept and used for the experiment in accordance with the ethics and regulation of animal experiments of Pharmaceutical Sciences, Shandong University, China. The work described has been carried out in accordance with The Code of Ethics of the World Medical Association Declaration of Helsinki for experiments. Abbreviation: CHOL, cholesterol. According to the preparation process of the ethanol injection method, other conditions were fixed to change the single factor dosage amount, CHOL dosage, sodium deoxycholate dosage, hydration speed, hydration temperature, hydration time, water injection speed , and the encapsulation efficiency EE was mainly investigated considering the particle size, morphology, stability, and uniformity of the nanoparticles, and screening out the factors that have significant effects for the orthogonal design.

The supernatant was filtered through a 0. The mobile phases were 0. When the gel is placed between the stationary plate and rotated cone, the shear rate ranged from 0. Kunming strain mice were randomly divided into two treatment groups, 4 mice in each group. The skin on the back was quickly excised, and the subcutaneous tissue was removed, washed in normal saline and dried using filter paper. Skin samples needed to be prepared at the time of use and confirmed by microscopic observation to show no damage.

Other methods like radiotracers 17 , 18 and electrochemical methods 19 , 20 could also be used to pre-screen skin. The exposed back skin was cleaned with saline and confirmed to show no damage. Using the same body control method, both the intact skin of rabbits and damaged skin of rabbits were given 0. The Draize scale was applied to evaluate the skin irritation, and irritation scores between 0 and 4 were used to grade the stimulus intensity, which ranged from no response to a severe response.

In vivo Pharmacokinetic Study The Kunming mice were anesthetized and depilated according to the method of 2. The circular filter paper with a diameter of 0. The wound area was measured every day.

Meanwhile, the wound inflammatory reaction, wound scarring time, healing time and rate of scar formation were recorded. After all the treatments, the Kunming mice were sacrificed and the skins of the mice were removed according to the method of 2. Finally, the skin was sliced with a paraffin slicer and analyzed using the Olympus VS panoramic digital slice scanning microscope Tokyo, Japan in the bright-field mode for scanning HE section analysis.

The larger the stirring speed is, the better the hydration effect is Figure 2A. As the amount of ethanol increased, the particle size of the alcohol body also became larger Figure 2C. From the transmission electron micrograph, the ethosomes containing a higher concentration of ethanol were more likely to be broken or polymerized. It was reported that the surfactant sodium deoxycholate changed the filling properties of the lipid in the bilayer, resulting in higher deformability, and it could be inserted between the lipid bilayers, resulting in a lower phase transition temperature of the skin lipid.

The optimal prescription was screened by orthogonal experiment using the encapsulation efficiency as an indicator. As the shear rate increased, the slope of the shear stress-shear rate curve decreased gradually, indicating that the viscosity of the formulation decreased and the gel exhibited pseudoplastic flow.

When the shear rate was 0. Under the scanning condition of SU 5. The size of the ethosomes was equal to the particle size measured under transmission electron microscopy, indicating that it was not significantly changeable for ethosomes in the morphology and size of the gel matrix after freeze drying. Regression was performed to fit zero-order, first-order, Higuchi and Weibull infiltration behavioral dynamics equations based on the relevant data.

During 0. Additionally, due to individual differences in the body weight and skin thickness of Kunming mice, the correlation coefficient can be appropriately reduced considering that the ripple factor is large, and a correlation coefficient below 0. Rabbits are highly sensitive to skin irritation and are easy to feed in the laboratory.

Thus, rabbits are widely used in skin penetration studies to predict human skin irritation and determine the safety. The phospholipids, CHOL and ethanol used in the preparation of ethosomal gel were mild, a finding consistent with the drug design principle of Quality by Design QbD. Table 2 Time of Wound Healing, Time of Forming Scab and the Percentage of the Scar on the Healing Wound After Administering Different Pharmaceutical Preparations Figure 5 Kunming mice administrated with different gel for 15 days have different degrees of wound healing A and the photomicrographs of the healed skin structure of using different preparations B.

In Figure 5B, the black arow indicated the degree of skin thickening, the red arow indicated new capillaries and the yellow arrow showed embolization and localized parakeratosis. Histopathology Examination Combined with the previous research results, we speculated that the nanodelivery drug system could make more drug pass through the skin stratum corneum and form drug depots in the deep layer, thus effectively promoting the effect of wound healing.

Photographs of hematoxylin and eosin staining for repaired skin administered with different formulations are illustrated in Figure 5B. As indicated by the black arrow, the damaged skin showed a degree of thickening, but the blank control group was not obvious.

Conclusion Although macromolecular protein drugs have attracted much attention due to their high biological activity, they have low skin permeability and easily cause skin irritation in TDDSs because of their large molecular weight and easy inactivation. We hypothesized that nanotechnology-mediated TDDSs can provide some help. The preparation of the ethosomes without ultrasonic disruption or liposome extrusion was simple.

The ethosomes showed good physical and chemical properties, such as a uniform particle size and complete morphology. We have demonstrated their transdermal release rate in vitro and drug effects in vivo through a series of experiments. Based on the experimental results, we observed that the ethosomal gel formulation has a better drug transdermal rate than the free drug group and significantly shortens the time of wound skin healing.

Skin irritation experiments further determined that the ethosomal gel has excellent biocompatibility. HE staining showed that the ethosomal gel preparation with loaded drug can promote skin wound healing.

Combining the above results, we conclude that this nano drug delivery system for the transdermal administration of macromolecular protein drugs has excellent clinical application potential and provides a possible good design for ethosomal gels with various transdermal delivery drugs e. China No. Disclosure The authors report no conflicts of interest in this work.

References 1. Thymosin beta4: structure, function, and biological properties supporting current and future clinical applications. Ann N Y Acad Sci. Ther Deliv. Approaches for breaking the barriers of drug permeation through transdermal drug delivery.

J Control Release. PVA cryogel as model hydrogel for iontophoretic transdermal drug delivery investigations. Colloids Surf B Biointerfaces. Slowly dissolving intradermal microneedles. Nat Biomed Eng. Mechanistic insights of the enhancement effect of sorbitan monooleate on olanzapine transdermal patch both in release and percutaneous absorption processes. Eur J Pharm Sci. Nanoparticle assisted solvent selective transdermal combination therapy of curcumin and 5-flurouracil for efficient cancer treatment.

Carbohydr Polym. Transdermal delivery from liposomal formulations - evolution of the technology over the last three decades. Mechanism of transdermal permeation promotion of lipophilic drugs by ethosomes.

Int J Nanomedicine. Nanovesicular carriers as alternative drug delivery systems: ethosomes in focus. Expert Opin Drug Deliv. Investigate the control release effect of ion-pair in the development of escitalopram transdermal patch using FT-IR spectroscopy, molecular modeling and thermal analysis. Int J Pharm. Comparison of 5-aminolevulinic acid-encapsulated liposome versus ethosome for skin delivery for photodynamic therapy.

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Ethosomes could enhance cell membrane fluidity and reduce epidermal membrane density to make macromolecular drugs through the stratum corneum into the deeper layers of the skin easily. Methods: We used the orthogonal method to optimize the formulation of the ethosome preparation prepared by the ethonal infusion method. Ethosomal gels were characterized by using different analytical methods. Transdermal release rate in vitro have been demonstrated in Franz diffusion cells and the efficacy of drug-loaded nanocarriers in vivo was investigated in a mouse model.

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