scholarly journals Plumbagin-Loaded Glycerosome Gel as Topical Delivery System for Skin Cancer Therapy

Polymers ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 923
Author(s):  
Shadab Md ◽  
Nabil A. Alhakamy ◽  
Hibah M. Aldawsari ◽  
Mohammad Husain ◽  
Nazia Khan ◽  
...  
Keyword(s):  
Skin Cancer ◽  
Zeta Potential ◽  
Skin Permeation ◽  
Entrapment Efficiency ◽  
Aqueous Solubility ◽  
Skin Layer ◽  
Vesicle Size ◽  
Cytotoxicity Activities

Plumbagin (PLM) is a phytochemical which has shown cytotoxicity against of cancer cells both in vitro and in vivo. However, the clinical application of PLM has been hindered due to poor aqueous solubility and low bioavailability. The aim of the present study was to develop, optimize and evaluate PLM-loaded glycerosome (GM) gel and compare with conventional liposome (CL) for therapeutic efficacy against skin cancer. The GM formulations were optimized by employing design expert software by 3-level 3-factor design. The prepared GMs were characterized in vitro for vesicle size, size distribution, zeta potential, vesicle deformability, drug release, skin permeation, retention, texture, antioxidant and cytotoxicity activities. The optimized formulation showed a vesicle size of 119.20 ± 15.67 nm with a polydispersity index (PDI) of 0.145 ± 0.02, the zeta potential of −27 ± 5.12 mV and entrapment efficiency of 76.42 ± 9.98%. The optimized PLM-loaded GM formulation was transformed into a pre-formed gel which was prepared using Carbopol 934 polymer. The drug diffusion fluxes of CL gel and GM-loaded gel were 23.31 ±6.0 and 79.43 ± 12.43 µg/ cm2/h, respectively. The result of texture analysis revealed the adequate hardness, cohesiveness, consistency, and viscosity of the developed GM-loaded gel compared to CL gel. The confocal images showed that glycerosomal gel has deeper skin layer penetration as compared to the control solution. GM-loaded gel treated rat skin showed significantly (p < 0.05) higher drug accumulation in the dermis, higher cytotoxicity and higher antioxidant activity as compared to CL gel and PLM suspension. Thus, findings revealed that novel GM-loaded gel could be potential carriers for therapeutic intervention in skin cancer.

scholarly journals Formulation, Development and Evaluation of Ibuprofen Loaded Nano-transferosomal Gel for the Treatment of Psoriasis

2019 ◽  
pp. 1-8
Author(s):  
Marwa H. Abdallah ◽  
Amr S. Abu Lila ◽  
Md. Khalid Anwer ◽  
El-Sayed Khafagy ◽  
Muqtader Mohammad ◽  
...  
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Formulation Development ◽  
In Vitro Drug Release ◽  
Vesicle Size

The present work was aimed to develop a transferosomal gel of ibuprofen (IBU) for the amelioration of psoriasis like inflammation. Three formulation of IBU loaded transferosomes (TFs1-TFs3) were prepared using different proportions of lipid (phospholipon 90H) and surfactant (tween 80) and further evaluated for vesicle size, zeta potential (ZP), entrapment efficiency and in vitro drug release. The IBU loaded transferosomes (TFs2) was optimized with vesicle size (217±8.4 nm), PDI (0.102), ZP (-31.5±4.3 mV), entrapment efficiency (88.4±6.9%) and drug loading (44.2±2.9%). Further, the optimized IBU loaded transferosomes (TFs2) was incorporated into 1% carbopol 934 gel base and characterized for homogeneity, extrudability, viscosity and drug content. The in vivo pharmacodynamic study of gel exhibited reduction in psoriasis like inflammation in mice. The ibuprofen loaded transferosomal gel was successfully developed and has shown the potential to be a new therapy against psoriasis like inflammation.

scholarly journals Development and Optimization of Proniosomal Gel Containing Etodolac: In-vitro, Ex-vivo and In-vivo Evaluation

2021 ◽  
Vol 62 (3) ◽  
pp. 290-304
Author(s):  
Moreshwar Patil ◽  
Prashant Pandit ◽  
Pavan Udavant ◽  
Sandeep Sonawane ◽  
Deepak Bhambere
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
In Vivo Evaluation ◽  
Vesicle Size ◽  
Skin Delivery ◽  
The Stability

Introduction: Etodolac is used in the treatment of acute pain and inflammation. It has low solubility because of high hydrophobicity and it is reported that upon oral administration shows gastric disturbances. This encourages the development of topical vesicular formulation. Method: In this work we used coacervation-phase separation method for the development of etodolac loaded vesicular system by using non-ionic surfactants, cholesterol and soya lecithin. Central composite design (rotatble) was used to optimize the concentrations of soy lecithin, surfactant and cholesterol. The prepared formulations were characterized by number of vesicles formed, vesicle size, zeta potential, entrapment efficiency, in-vitro permeation, ex-vivo permeation and anti-inflammatory study. Results: Etodolac was successfully entrapped in all formulations having efficiency in the range of 74.36% to 90.85%, which was more at 4 °C than room temperature. When hydrated with water; niosome in the range of 54 to 141 (per cubic mm) were spontaneously produced. The results of in-vitro diffusion study revealed that etodolac was released in the range of 71.86 to 97.16% over a period of 24 hrs. The average vesicle size of optimized formulation was found 211.9 nm with PDI of 0.5. The observed responses i.e. % encapsulation efficiency and drug release were 74.12 and 95.08 respectively. The zeta potential was -19.4mV revealed the stability of formulation which was further confirmed by no changes in drug content and drug release after stability studies. The % inhibition in paw volume was 40.52% and 43.61% for test and marketed proniosomal gel. Conclusion: Proniosomal gel formulation was stable and could enhance skin delivery of etodolac because of excellent permeation capability of vesicular system.

Nanostructured Ethosomal Gel Loaded with Arctostaphylos uva-ursi extract; In-vitro/In-vivo Evaluation as a Cosmeceutical Product

2021 ◽  
Vol 18 ◽  
Author(s):  
Nayla Javed ◽  
Shakeel Ijaz ◽  
Naveed Akhtar ◽  
Haji Muhammad Shoaib Khan
Keyword(s):  
Zeta Potential ◽  
Biological Activities ◽  
Skin Permeation ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Potential Candidate ◽  
Skin Rejuvenation ◽  
In Vivo Evaluation

Background: Arctostaphylos uva-ursi (AUU) being rich in polyphenols and arbutin is known to have promising biological activities and can be a potential candidate as a cosmaceutical. Ethosomes encourage the formation of lamellar-shaped vesicles with improved solubility and entrapment of many drugs including plant extracts. Objective: The objective of this work was to develop an optimized nanostructured ethosomal gel formulation loaded with AUU extract and evaluated for skin rejuvenation and depigmentation. Methods: AUU extract was tested for phenolic and flavonoid content, radical scavenging potential, reducing power activity, and in-vitro SPF (sun protection factor) estimation. AUU loaded 12 formulations were prepared and characterized by SEM (scanning electron microscopy), vesicular size, zeta potential, and entrapment efficiency (%EE). The optimized formulation was subjected to non-invasive in-vivo investigations after incorporating it into the gel system and ensuring its stability and skin permeation. Results: Ethosomal vesicles were spherical in shape and Zeta size, zeta potential, PDI (polydispersity index), % EE and in-vitro skin permeation of optimized formulation (F3) were found to be 114.7nm, -18.9mV, 0.492, 97.51±0.023%, and 79.88±0.013% respectively. AUU loaded ethosomal gel formulation was stable physicochemically and exhibited non-Newtonian behavior rheologically. Moreover, it significantly reduced skin erythema, melanin as well as sebum level and improved skin hydration and elasticity. Conclusion: A stable AUU based ethosomal gel formulation could be a better vehicle for phytoextracts than conventional formulations for cosmeceutical applications such as for skin rejuvenation and depigmentation etc.

scholarly journals Improving the Antitumor Activity and Bioavailability of Sonidegib for the Treatment of Skin Cancer

Pharmaceutics ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 1560
Author(s):  
Amr Gamal ◽  
Haitham Saeed ◽  
Fatma I. Abo El-Ela ◽  
Heba F. Salem
Keyword(s):  
Steady State ◽  
Skin Cancer ◽  
Entrapment Efficiency ◽  
The United States ◽  
Relative Bioavailability ◽  
Passive Targeting ◽  
Therapeutic Benefits ◽  
Steady State Flux

Throughout the United States and the world, skin cancer is the most frequent form of cancer. Sonidegib (SNG) is a hedgehog inhibitor that has been used for skin cancer treatment. However, SNG has low bioavailability and is associated with resistance. The focus of this work is to enhance bioavailability, anti-tumor efficacy and targeting of SNG via developing ethosome gel as a potential treatment for skin cancer. SNG-loaded ethosomes formulation was prepared and characterized in vitro by %entrapment efficiency (%EE), vesicle size, morphology, %release and steady-state flux. The results showed that the prepared formulation was spherical nanovesicles with a %EE of 85.4 ± 0.57%, a particle size of 199.53 ± 4.51 nm and a steady-state flux of 5.58 ± 0.08 µg/cm2/h. In addition, SNG-loaded ethosomes formulation was incorporated into carbopol gel to study the anti-tumor efficacy, localization and bioavailability in vivo. Compared with oral SNG, the formulation showed 3.18 times higher relative bioavailability and consequently significant anti-tumor activity. In addition, this formulation showed a higher rate of SNG penetration in the skin’s deep layers and passive targeting in tumor cells. Briefly, SNG-loaded ethosome gel can produce desirable therapeutic benefits for treatment of skin cancer.

scholarly journals Enhanced Therapeutic Efficacy of Vincristine Sulfate for Lymphoma Using Niosome-Based Drug Delivery

2020 ◽  
Vol 15 (3) ◽  
Author(s):  
Mohammad Reza Mehrabi ◽  
Mohammad Ali Shokrgozar ◽  
Tayebeh Toliyat ◽  
Masoomeh Shirzad ◽  
Azadeh Izadyari ◽  
...  
Keyword(s):  
Side Effects ◽  
Zeta Potential ◽  
Anticancer Activity ◽  
Performance Test ◽  
Entrapment Efficiency ◽  
Aqueous Solubility ◽  
Diffusion Method ◽  
Vincristine Sulfate ◽  
Lymphoma Cells

: Clinical application of vincristine sulfate as a chemotherapeutic agent is limited because of its low aqueous solubility and severe side effects. This study aimed to improve the bioavailability and reduce side effects of vincristine sulfate through entrapping in PEGylated niosomes. We evaluated the anticancer activity of PEGylated niosomal vincristine sulfate (PEG-nVCR) in a mouse model of lymphoma induced by BCL1 clone 5B1b cell line. PEG-nVCR was prepared by the thin-film hydration method. The prepared niosomes were characterized by size, zeta potential, and entrapment efficiency. The drug release pattern, neurotoxicity experiment, and in vivo anticancer activity of PEG-nVCR were evaluated by the dialysis diffusion method, rotarod performance test, and flow cytometry, respectively. The mean particle size, zeta potential, and entrapment efficiency of nisomes were obtained around 220 nm, -19 mV, and 81%, respectively. A sustained release behavior was indicated by PEG-nVCR so that the maximum release of VCR from niosomes reached to 69% after 36h of incubation. After the treatment of mice by different formulations, a significant reduction in lymphoma cells in the spleen was obtained for the PEG-nVCR, as compared to the free vincristine sulfate. In the neurotoxicity experiment, a 2.5-fold lower motor incoordination effect was observed for the PEG-nVCR group with respect to the free VCR group. According to these findings, it can be concluded that the PEGylated niosomal formulation could be a suitable carrier for the delivery of VCR to the lymphoma cells or other related cancer cells.

Investigating the potential of Quercetin enthused nano lipoidal system for the management of dermatitis

2021 ◽  
pp. 6516-6526
Author(s):  
Deepti Dwivedi ◽  
Shubham Pandey ◽  
Shafaque Asif ◽  
Vineet Awasthi ◽  
Gurjeet Kaur ◽  
...  
Keyword(s):  
Zeta Potential ◽  
Skin Permeation ◽  
Research Work ◽  
Entrapment Efficiency ◽  
Laser Scanning Microscopy ◽  
Polydispersity Index ◽  
In Vivo Studies ◽  
Confocal Laser ◽  
Skin Retention

Objective: The present research work was undertaken to develop quercetin enthused nanolipoidal systems and its characterization. The objective was to investigate potential of prepared system in the management of DNCB induced dermatitis. Method: Nanolipoidal system was prepared in different combinations with quercetin, L-α phosphatidylcholine (SPC) and ethanol and characterized for particle size, polydispersity index (PDI), zeta potential, drug entrapment efficiency, percentage drug release, skin retention and skin permeation. Selected batches were further incorporated into Carbopol 934 base gel. The vesicles were in size range 324.19-359 nm while polydispersity index (PDI) ranges from 0.241-0.554 and for zeta potential, it was from -26.33 to -39.3 nm. Entrapment efficiency was from 23.77-94.68 %. Confocal laser scanning microscopy showed penetration depth of rhodamine enthused ethosome across rat skin up to 45.23 µm which was significantly higher than the rhodamine solution (10 µm). In dinitrochlorobenzene (DNCB) induced mice dermatitis model histopathology study showed a marked decrease in amount of inflammatory cell nucleus in mice treated with quercetin loaded ethosomal gel followed by 76.13% decrease in-ear swelling and ear mass respectively in morphology study. The conventional marketed formulation showed a nominal decrease in epidermal thickness. Further Primary irritation index was less than 0.4 indicating negligible irritation in all the groups. Results: The optimized formulation F6 with SPC and ethanol in the ratio of 20:80 displayed the highest drug content and entrapment efficiency of 94.68±1.14%. PDI was 0.241±0.11 and skin retention 7.7%. Batch F6 with vesicle size and zeta potential of 324.9±19 nm and -26.33 mV, respectively, was incorporated in Carbopol 934 base gel and the prepared gel was evaluated for morphology, spreadability, in vitro, ex vivo release study, and kinetics study and in vivo studies. Conclusion: The present study revealed that the developed ethosomal gel can be used for enhanced delivery of Quercetin via skin. The in vitro studies indicated that the gel serves as an efficient carrier for Quercetin. It showed its effectiveness in the management of dermatitis. Further, Quercetin loaded nanoethosomal gel formulation can be viewed as a promising drug delivery system for the management of dermatitis.

scholarly journals Transcutol® P Containing SLNs for Improving 8-Methoxypsoralen Skin Delivery

Pharmaceutics ◽  
2020 ◽  
Vol 12 (10) ◽  
pp. 973
Author(s):  
Giulia Pitzanti ◽  
Antonella Rosa ◽  
Mariella Nieddu ◽  
Donatella Valenti ◽  
Rosa Pireddu ◽  
...  
Keyword(s):  
Skin Permeation ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Skin Layer ◽  
Skin Permeability ◽  
Puva Therapy ◽  
Ultraviolet A ◽  
3T3 Fibroblasts ◽  
Skin Delivery

Topical psoralens plus ultraviolet A radiation (PUVA) therapy consists in the topical application of 8-methoxypsoralen (8-MOP) followed by the skin irradiation with ultraviolet A radiation. The employment of classical 8-MOP vehicles in topical PUVA therapy is associated with poor skin deposition and weak skin permeability of psoralens, thus requiring frequent drug administration. The aim of the present work was to formulate solid lipid nanoparticles (SLNs) able to increase the skin permeation of 8-MOP. For this purpose, the penetration enhancer Transcutol® P (TRC) was added to the SLN formulation. SLNs were characterized with respect to size, polydispersity index, zeta potential, entrapment efficiency, morphology, stability, and biocompatibility. Finally, 8-MOP skin diffusion and distribution within the skin layers was investigated using Franz cells and newborn pig skin. Freshly prepared nanoparticles showed spherical shape, mean diameters ranging between 120 and 133 nm, a fairly narrow size distribution, highly negative ζ potential values, and high entrapment efficiency. Empty and loaded formulations were almost stable over 30 days. In vitro penetration and permeation studies demonstrated a greater 8-MOP accumulation in each skin layer after SLN TRC 2% and TRC 4% application than that after SLN TRC 0% application. Finally, the results of experiments on 3T3 fibroblasts showed that the incorporation of TRC into SLNs could enhance the cellular uptake of nanoparticles, but it did not increase their cytotoxicity.

Prolonged Anti-Inflammatory Activity of Topical Melatonin by Niosomal Encapsulation

2014 ◽  
Vol 902 ◽  
pp. 70-75 ◽  
Author(s):  
Aroonsri Priprem ◽  
Vassana Netweera ◽  
Pramote Mahakunakorn ◽  
Nutjaree Pratheepawanit Johns ◽  
Jeffrey Roy Johns
Keyword(s):  
Skin Permeation ◽  
Entrapment Efficiency ◽  
Rapid Decline ◽  
Tail Flick ◽  
Tail Flick Test ◽  
Topical Gel ◽  
Anti Inflammatory ◽  
Average Size

Melatonin, encapsulated and non-encapsulated, in a topical gel, was comparatively investigated for its in vitro permeation and in vivo anti-inflammatory properties. An average size of the melatonin-encapsulated niosomes of 197 nm with a zeta potential of-78.8 mV and an entrapment efficiency of 92.7% was incorporated into a gel base. In vitro skin permeation of the same gel base incorporated with non-encapsulated melatonin or melatonin niosomes at 5% was comparatively evaluated through porcine skin using Franz diffusion cells and analyzed by spectroflurometry at λex 278 and λem 348 nm. From the same gel base, the permeation rate of non-encapsulated melatonin was about 2.5 times greater than that of melatonin-encapsulated niosomes. In comparison to piroxicam gel and hydrocortisone cream used as the positive controls, topical applications of melatonin and melatonin niosome gels tested in croton oil-induced ear edema in mice suggested that its anti-inflammatory activities were prolonged by the niosomal encapsulation. Similarly, analgesic effect of melatonin was prolonged by niosomal encapsulation using tail flick test in mice. Therefore, its immediate permeation through the skin was retarded by niosomal encapsulation which could also prolong its rapid decline in exerting anti-inflammatory and analgesic activities in vivo.

scholarly journals DERMAL DELIVERY OF DOCETAXEL LOADED NANO LIQUID CRYSTALS FOR THE TREATMENT OF SKIN CANCER

2019 ◽  
pp. 188-193 ◽  
Author(s):  
ARTI MAJUMDAR ◽  
NIDHI DUBEY ◽  
NITIN DUBEY
Keyword(s):  
Liquid Crystals ◽  
Skin Cancer ◽  
Zeta Potential ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Cell Uptake ◽  
Diffusion Method ◽  
Average Particle ◽  
Uptake Study

Objective: The aim of the present study is to develop docetaxel-loaded nano liquid crystals (NLCs) to enhanced and effective delivery of the drug to the skin cancer. Methods: NLCs bearing docetaxel were prepared by an emulsification solvent diffusion method. The formulated NLCs were characterized for average particle size, polydispersity index (PDI) Zeta potential, entrapment efficiency and in vitro drug release study. The prepared formulations were studied for it's in vitro cell line and cell uptake study. Results: It was revealed that the average size of NLCs was found 178.3±5.07, PDI was 0.189, percent entrapment efficiency was found 71.3±2.49 and Zeta potential was found-17.3±2.4. In vitro release determined by Franz diffusion cell was found 61.6±3.2% after 72 hr. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay shows that Docetaxel loaded NLCs were giving more cytotoxicity as compared to the plain drug. The cell uptake study was found enhanced uptake of fluorescein isothiocyanate (FITC) loaded NLCs in comparison to plain FITC. Docetaxel and docetaxel-loaded NLCs showed 28.3±0.3 and 39.3±1.3 growth inhibition respectively after 48h upon incubation at 0.5 µg/ml concentration (p<0.05). Conclusion: The result of the studies was concluded that NLCs can be used as impending drug delivery system which may enhance the drug uptake and maintain the drug level for longer period of time and it is potential carrier system which can be used for the treatment of skin diseases like cancer.

Optimized Preparation of Capsaicin-Loaded Nanoparticles Gel by Box-Behnken Design

2014 ◽  
Vol 1061-1062 ◽  
pp. 359-368 ◽  
Author(s):  
Mei Ling Tang ◽  
Li Hua Chen ◽  
Dong Sheng Zhou ◽  
Wei Feng Zhu ◽  
Yong Mei Guan ◽  
...  
Keyword(s):  
Skin Permeation ◽  
Skin Irritation ◽  
Morphological Characteristics ◽  
Entrapment Efficiency ◽  
Box Behnken Design ◽  
Irritation Test ◽  
Predicted Values ◽  
Skin Irritation Test

A three-factor three-level Box-Behnken design(BBD) was employed to optimize capsaicin-loaded nanoparticles(Cap-NPs), and its properties in vitro and in vivo were evaluated. Particle size, morphological characteristics, entrapment efficiency of Cap-NPs were investigated respectively by Zetasizer, H7000 TEM and HPLC. Release, skin permeation and skin irritation test were investigated on mouse and rabbits. The predicted values of Cap-NPs were 94.50±6.33% for entrapment efficiency(EE) and 170.30±7.81 nm for particle mean diameter(PMD) under optimal conditions which were 346.33 bar (homogenization pressure, X1), 4.67 min(homogenization time, X2), and 15421.42 rpm (shear rate, X3). The in vitro permeation study showed that capsaicin permeability in NPs-gel was a 2.80-fold greater flux values than conventional ointment after 24 h. Cap-NPs-gel produce no observable skin irritation in rabbits within 72h. The optimized Cap-NPs-gel would be a good candidate for transdermal delivery.

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