Development of cyclosporine-loaded nanoemulsion for topical treatment of psoriasis

Psoriasis is an autoimmune disease in which the symptoms are obviously appeared on the patient's body with thick, red/ salmon colour and dry patches. Clinically, topical treatment has been the first-line treatment for psoriasis, whether or not the systemic and phototherapy is required. Currently, cyclosporine is one of the standard oral medications used for moderate to a severe case of psoriasis. However, through oral delivery, it cannot be used for a long period and causes bad effects. Thus, a new delivery system of cyclosporine is in need to be developed to overcome its toxic effects by skipping the first pass body metabolism. A nanoemulsion colloidal system, as the main carrier for big, non-water-soluble cyclosporine, is believed could help in the delivery of activities through the stratum corneum of the skin layer. Nanoemulsion system, which mainly consists of oil phase (a mixture of virgin coconut oil, nutmeg oil, and cyclosporine), aqueous phase, and surfactant, was successfully being developed by using Mixture Experimental Design optimization tool with droplet size range between 110-160 nm. Stability studies were carried out with respect to; pH, storage at different temperatures, coalescence and Ostwald ripening mechanism, free-thaw cycle, and FTIR analysis. From the obtained results, this newly-developed nanoemulsion containing cyclosporine was proven to be stable and successfully maintained its physicochemical characteristics even after 3 months of storage at 4°C and 25°C temperature. Ostwald ripening mechanism contributed to the instability of the system at 45°C of storage. Introduction of standard cyclosporine, blank nanoemulsion, and nanoemulsion containing cyclosporine to the HaCaT cells in the treatment of MTT assay study has confirmed the safety of the nanoemulsion. Permeation study of the newly-developed nanoemulsion containing cyclosporine showed it was best fitted the Korsmeyer-Peppas kinetic model. In addition, the transepidermal water loss and hydration studies proved the efficacy of cyclosporine-loaded nanoemulsion in increasing the water storage of the volunteers’ normal skin after 3h of application.

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Facial Treatment with 3-O-Cetyl Ascorbic Acid for Improvement of Skin Texture: Uptake, Effectiveness, and In Vitro Carcinogenicity Assessment

Cosmetics ◽

10.3390/cosmetics8020038 ◽

2021 ◽

Vol 8 (2) ◽

pp. 38

Author(s):

Natsumi Doi ◽

Yoshifumi Yamada ◽

Misaki Toyoshima ◽

Yuki Kondo ◽

Koichi Nakaoji ◽

...

Keyword(s):

Ascorbic Acid ◽

Topical Treatment ◽

Secondary Ion Mass Spectrometry ◽

Biological Activities ◽

Normal Skin ◽

Water Soluble ◽

Tape Stripping ◽

Healthy Human ◽

Lipophilic Derivative

Ascorbic acid (AA) is a water-soluble vitamin that is found at high concentrations in normal skin. The important and well-known benefits of using AA in skin health include the stimulation of collagen synthesis and the assistance of protection against photo-oxidative damages. To maintain stability and improve drug delivery to the active site, a variety of AA derivatives have been chemically synthesized. Among these compounds, we focus here on a lipophilic derivative, 3-O-cetyl ascorbic acid (3-CetylAA), which remains poorly characterized for cosmetic applications. Uptake analysis in three healthy human volunteers’ skin was conducted using a serial tape-stripping technique detecting 3-CetylAA (on average, 128 ± 27 pmol per µg) in the stratum corneum after a 5-h topical treatment when treated with 25 mM 3-CetylAA-containing cream for 13 days twice daily and continuously. Time-of-flight secondary ion mass spectrometry (ToF-SIMS) imaging of vertical cryosections of pig skin revealed the presence of 3-CetylAA in the epidermal layer after topical treatment with 3-CetylAA-containing cream. In sun-exposed human skin, 3-CetylAA improved the texture after treatment with 25 mM 3-CetylAA-containing cream for 4 weeks or more when used twice daily or continuously. An in vitro transformation assay using BALB/c 3T3 A31-1-1 cells demonstrated that 10 µM 3-CetylAA, which is the same concentration exhibited in vitro biological activities in another lipophilic AA derivative, 2-O-octadecyl ascorbic acid, was non-carcinogenic and did not potentiate the UVC-induced transformation frequency when applied for 3 days after UVC irradiation. These results demonstrate that 3-CetylAA is a promising candidate as a lipophilic derivative of AA for cosmetic purposes.

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Microsponges: An Overview

International Journal of Drug Delivery Technology ◽

10.25258/ijddt.v4i4.8860 ◽

2017 ◽

Vol 4 (4) ◽

Author(s):

Hamid Hussain ◽

Divya Juyal ◽

Archana Dhyani

Keyword(s):

Controlled Release ◽

Delivery System ◽

Oral Delivery ◽

Active Agent ◽

Topical Delivery ◽

Water Soluble ◽

Wide Range ◽

Porous Beads

Microsponge and Nanosponge delivery System was originally developed for topical delivery of drugs can also be used for controlled oral delivery of drugs using water soluble and bioerodible polymers. Microsponge delivery system (MDS) can entrap wide range of drugs and then release them onto the skin over a time by difussion mechanism to the skin. It is a unique technology for the controlled release of topical agents and consists of nano or micro porous beads loaded with active agent and also use for oral delivery of drugs using bioerodible polymers.

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Fenofibrate Solid Dispersion for Improving Oral Bioavailability: Preparation, and Characterization and in vivo Evaluation

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2020.13.5.7 ◽

2020 ◽

Vol 13 (5) ◽

pp. 5102-5109

Author(s):

Venu Madhav K ◽

Somnath De ◽

Chandra Shekar Bonagiri ◽

Sridhar Babu Gummadi

Keyword(s):

Oral Bioavailability ◽

Oral Delivery ◽

Solid Dispersions ◽

In Vitro Release ◽

Aqueous Solubility ◽

Water Soluble ◽

Scanning Calorimetry ◽

In Vivo Evaluation

Fenofibrate (FN) is used in the treatment of hypercholesterolemia. It shows poor dissolution and poor oral bioavailability after oral administration due to high liphophilicity and low aqueous solubility. Hence, solid dispersions (SDs) of FN (FN-SDs) were develop that might enhance the dissolution and subsequently oral bioavailability. FN-SDs were prepared by solvent casting method using different carriers (PEG 4000, PEG 6000, β cyclodextrin and HP β cyclodextrin) in different proportions (0.25%, 0.5%, 0.75% and 1% w/v). FN-SDs were evaluated solubility, assay and in vitro release studies for the optimization of SD formulation. Differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM) analysis was performed for crystalline and morphology analysis, respectively. Further, optimized FN-SD formulation evaluated for pharmacokinetic performance in Wistar rats, in vivo in comparison with FN suspension. From the results, FN-SD3 and FN-SD6 have showed 102.9 ±1.3% and 105.5±3.1% drug release, respectively in 2 h. DSC and PXRD studies revealed that conversion of crystalline to amorphous nature of FN from FT-SD formulation. SEM studies revealed the change in the orientation of FN when incorporated in SDs. The oral bioavailability FN-SD3 and FN-SD6 formulations exhibited 2.5-folds and 3.1-folds improvement when compared to FN suspension as control. Overall, SD of FN could be considered as an alternative dosage form for the enhancement of oral delivery of poorly water-soluble FN.

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Functionally Engineered Nanosized Particles in Pharmaceutics: Improved Oral Delivery of Poorly Water-soluble Drugs

Current Pharmaceutical Design ◽

10.2174/1381612811319350004 ◽

2013 ◽

Vol 19 (35) ◽

pp. 6259-6269 ◽

Cited By ~ 7

Author(s):

Tetsuya Ozeki ◽

Tatsuaki Tagami

Keyword(s):

Oral Delivery ◽

Water Soluble ◽

Nanosized Particles ◽

Poorly Water Soluble Drugs ◽

Water Soluble Drugs ◽

Poorly Water Soluble

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Development of biodegradable porous starch foam for improving oral delivery of poorly water soluble drugs

International Journal of Pharmaceutics ◽

10.1016/j.ijpharm.2010.09.040 ◽

2011 ◽

Vol 403 (1-2) ◽

pp. 162-169 ◽

Cited By ~ 75

Author(s):

Chao Wu ◽

Zhongyan Wang ◽

Zhuangzhi Zhi ◽

Tongying Jiang ◽

Jinghai Zhang ◽

...

Keyword(s):

Oral Delivery ◽

Water Soluble ◽

Poorly Water Soluble Drugs ◽

Water Soluble Drugs ◽

Poorly Water Soluble

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Polymeric Micelles, a Promising Drug Delivery System to Enhance Bioavailability of Poorly Water-Soluble Drugs

Journal of Drug Delivery ◽

10.1155/2013/340315 ◽

2013 ◽

Vol 2013 ◽

pp. 1-15 ◽

Cited By ~ 190

Author(s):

Wei Xu ◽

Peixue Ling ◽

Tianmin Zhang

Keyword(s):

Drug Delivery ◽

Residence Time ◽

Oral Delivery ◽

Polymeric Micelles ◽

Water Soluble ◽

Gi Tract ◽

Poorly Water Soluble Drugs ◽

Water Soluble Drugs ◽

Poorly Water Soluble ◽

Accepted Form

Oral administration is the most commonly used and readily accepted form of drug delivery; however, it is find that many drugs are difficult to attain enough bioavailability when administered via this route. Polymeric micelles (PMs) can overcome some limitations of the oral delivery acting as carriers able to enhance drug absorption, by providing (1) protection of the loaded drug from the harsh environment of the GI tract, (2) release of the drug in a controlled manner at target sites, (3) prolongation of the residence time in the gut by mucoadhesion, and (4) inhibition of efflux pumps to improve the drug accumulation. To explain the mechanisms for enhancement of oral bioavailability, we discussed the special stability of PMs, the controlled release properties of pH-sensitive PMs, the prolongation of residence time with mucoadhesive PMs, and the P-gp inhibitors commonly used in PMs, respectively. The primary purpose of this paper is to illustrate the potential of PMs for delivery of poorly water-soluble drugs with bioavailability being well maintained.

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SOLID DISPERSIONS: RESUSCITATING ORAL DELIVERY OF HYDROPHOBIC DRUGS

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2019.v12i3.29948 ◽

2019 ◽

pp. 213-217

Author(s):

RUCHI AGRAWAL ◽

ABID RAZA ◽

OM PRAKASH PATEL

Keyword(s):

Oral Delivery ◽

Solid Dispersions ◽

Water Soluble ◽

Future Trends ◽

Hydrophobic Drugs ◽

Poorly Water Soluble Drugs ◽

Advantages And Disadvantages ◽

Water Soluble Drugs ◽

Poorly Water Soluble ◽

Viable Method

Objective: This review article explores solid dispersions (SDs) as one of the suitable approaches to formulate poorly water-soluble drugs. The objective of this review on SD techniques is to explore their utility as a feasible, simple, and economically viable method for augmentation of dissolution of hydrophobic drugs. Methods: Various types of SDs are classified and compared. Use of surfactants to stabilize the SDs and their potential advantages and disadvantages has been discussed. Different techniques for preparing and evaluating SDs are appraised along with discussions on scalability and industrial production. Review of the current research on SD along with future trends is also offered. Results: Based on the various researches, SDs offer an efficient means of improving bioavailability while concurrently contributing to lower toxicity and dose-reduction. Conclusion: Solid-dispersions have been and continue to be one of the key technologies for solving the issue of poor solubility for newer hydrophobic molecules which are being discovered. This would give a new lease of life for such drugs enabling them to be delivered in an effective way.

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Impact of hygroscopic seeding on the initiation of precipitation formation: results of a hybrid bin microphysics parcel model

10.5194/acp-2021-506 ◽

2021 ◽

Author(s):

Istvan Geresdi ◽

Lulin Xue ◽

Sisi Chen ◽

Youssef Wehbe ◽

Roelof Bruintjes ◽

...

Keyword(s):

Size Distribution ◽

Drop Size ◽

Ostwald Ripening ◽

Drop Size Distribution ◽

Water Soluble ◽

Substantial Contribution ◽

Cloud Base ◽

Model Framework ◽

The Impact ◽

Precipitation Formation

Abstract. A hybrid bin microphysical scheme is developed in a parcel model framework to study how natural aerosol particles and different types of hygroscopic seeding materials affect the precipitation formation. A novel parameter is introduced to describe the impact of different seeding particles on the evolution of the drop size distribution. The results of more than 100 numerical experiments using the hybrid bin parcel model show that: (a) The Ostwald-ripening effect has a substantial contribution to the broadening of the drop size distribution near the cloud base. The efficiency of this effect increases as the updraft velocity decreases. (b) The efficiency of hygroscopic seeding is significant only if the size of the seeding particles is in the coarse particle size range. The presence of the water-soluble background coarse particles reduces the efficiency of the seeding. (c) The efficient broadening of the size distribution due to the seeding depends on the width of the size distribution of water drops in the control cases, but the relation is not as straightforward as in the case of the glaciogenic seeding.

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