Comparative efficacy of transdermal forms for alopecia therapy

Introduction. Alopecia is a polyetiological disorder characterized by hair loss and reducing their number per unit area. Baldness causes psychological and social discomfort to patients, in connection with what an important task is to develop formulations that are more effective than the reference agents.Aim. Investigate the possibility of applying the original substance Y in several dosage forms for the treatment of alopecia in comparison with reference drugs: minoxidil and burdock oil.Materials and methods. The research subject was the original substance Y, for which several dosage forms were made: gel, alcohol and oil compositions. The study on the effectiveness and safety of the developed formulations was carried out on 9 groups of male C57BL/6 mice. Depilation with further assessment of the percentage of hair follicles in the growth and resting phases was tested as a pre-clinical model of alopecia. In the study of the mechanism of action of substance Y, chemiluminescent assay was performed compared with natural antioxidant quercetin in the system luminol – 2,2'-azo-bis(2-amidinopropane)dihydrochloride, in potassium-phosphate buffer medium (pH = 7.4). Statistical processing of the results was carried out using two-way ANOVA using GraphPad Prism 8.0.2, USA software at the level of statistical significance of differences p < 0.05 and p < 0.005.Results and discussion. Based on the results of histological analysis and visual changes, it was found that the effectiveness of the topical forms of substance Y decreases in the following order: gel, alcohol form, oil composition. The use of a combination of the gel base with the test substance Y resulted to the appearance of a larger number of hair follicles in the growth phase than when using the reference preparation – 2 % minoxidil solution (the differences are statistically significant). Chemiluminescent assessment of antioxidant activity showed the lack of antioxidant effect in substance Y.Conclusion. The study combines two pharmaceutical profiles: technological and pharmacological. In the course of the experiments, the prospects of the gel form of the original substance Y for topical therapy of alopecia were shown. In the near future, it is planned to study the mechanism of action of substance Y, as well as registration of patent protection for a new drug.

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Topical Lipid Based Drug Delivery Systems for Skin Diseases: A Review

Current Drug Therapy ◽

10.2174/1574885513666181112153213 ◽

2020 ◽

Vol 15 (4) ◽

pp. 283-298

Author(s):

Suresh Kumar Sahu ◽

Rakesh Raj ◽

Pooja Mongia Raj ◽

Ram Alpana

Keyword(s):

Drug Delivery ◽

Skin Diseases ◽

Topical Therapy ◽

Skin Layer ◽

Dosage Forms ◽

Delivery Systems ◽

Systemic Side Effects ◽

Transcutaneous Delivery ◽

Topical Dosage ◽

Topical Dosage Forms

Treatment of skin ailments through systemic administration is limited due to toxicity and patients discomfort. Hence, lower risk of systemic side effects from topical dosage forms like ointments, creams, emulsions and gels is more preferred for the treatment of skin disease. Application of lipid based carriers in drug delivery in topical formulations has recently become one of the major approaches to improve drug permeation, safety, and effectiveness. These delivery systems include liposomes, ethosomes, transfersomes, Nanoemulsions (NEs), Solid Lipid Nanoparticles (SLNs) Nanostructured Lipid Carriers (NLCs) and micelles. Most of the liposomes and SLNs based products are in the market while some are under investigation. Transcutaneous delivery of therapeutics to the skin layer by novel lipid based carriers has enhanced topical therapy for the treatment of skin ailments. This article covers an overview of the lipid-based carriers for topical uses to alleviate skin diseases.

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Zosteriform Nevus Comedonicus

International Journal of Research in Pharmaceutical Sciences ◽

10.26452/ijrps.v11ispl4.4565 ◽

2020 ◽

Vol 11 (SPL4) ◽

pp. 2609-2612

Author(s):

Babbita S ◽

Thillaikkarasi A ◽

Sathyanarayanana R ◽

Narasimhalu CRV ◽

Sulochana Sonti

Keyword(s):

Topical Therapy ◽

Treatment Options ◽

Neck Region ◽

Surgical Excision ◽

Hair Follicles ◽

Treatment Modalities ◽

Developmental Defect ◽

Linear Distribution ◽

Head And Neck Region ◽

Typical Morphology

Nevus comedonicus is an uncommon cutaneous developmental defect of follicular apparatus characterized by unilateral and linear distribution of bundles of dilated hair follicles filled with keratin plugs. It is usually seen on the head and neck region, trunk and upper arm. This condition may be present at birth or can occur later in life. The term nevus comedonicus is a misnomer as there are no true comedones and is better termed as follicular keratotic nevus. It is also known as nevus zoniforme or nevus acneiformis unilateralis. There are two types of nevus comedonicus, namely inflammatory and non-inflammatory (non-pyogenic). When nevus comedonicus is manifested with other extracutaneous symptoms, it is termed as nevus comedonicus syndrome. Diagnosis is mainly clinical, based on history and typical morphology. As the disease runs a benign course, no aggressive treatment is required. Patients seek treatment, especially for cosmetic purposes and inflammatory type of lesions. Various treatment modalities like topical therapy, surgical excision, lasers are available and treatment options are individualized based on the size and extent of the lesion. We herein present a case of unilateral nevus comedonicus with no systemic associations in a 30-year-old female on her lower limb which is not a common site of occurrence.

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Factors Contributing to Intra-Individual Variation of Serum Constituents: 2. Effects of Exercise and Diet on Variation of Serum Constituents in Healthy Subjects

Clinical Chemistry ◽

10.1093/clinchem/19.12.1380 ◽

1973 ◽

Vol 19 (12) ◽

pp. 1380-1383 ◽

Cited By ~ 48

Author(s):

Bernard E Statland ◽

Per Winkel ◽

Henning Bokelund

Keyword(s):

Uric Acid ◽

Healthy Subjects ◽

Sodium Phosphate ◽

Statistical Significance ◽

Potassium Phosphate ◽

Strenuous Exercise ◽

Fasting State ◽

Total Lipids ◽

Physiological Factors ◽

Methodological Considerations

Abstract A previous report of within-day variation of serum constituents was based on values in healthy subjects who did not undergo strenuous exercise and who were in a fasting state. In this study we consider the effects of exercise and of a noon meal on the same serum constituents. The statistical significance (t-test) was computed on the basis of the ratios of values (after/before) on the day of exercise vs. the ratios on the nonexercise day, or, for the effect of meal, the ratios of values (after/before the noon meal) on the eating day vs. the ratios of values taken at the same hour on the fasting day. Significant effects seen after exercise (P <.05) included: potassium, phosphate, creatinine, total protein, albumin, uric acid, and alanine aminotransferase. After the noon meal, significant (P <.05) changes were seen for: sodium, phosphate, uric acid, iron, total lipids, alkaline phosphatase (phenyl phosphate substrate), and lactate dehydrogenase. The effects of eating on serum constituents are separated into (a) physiological factors and (b) methodological considerations.

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Determination of Terbutaline Sulfate in Dosage Forms by Liquid Chromatography with Electrochemical Detection

Journal of AOAC INTERNATIONAL ◽

10.1093/jaoac/70.6.974 ◽

1987 ◽

Vol 70 (6) ◽

pp. 974-976

Author(s):

William L Childress

Keyword(s):

Electrochemical Detection ◽

Silver Chloride ◽

Potassium Phosphate ◽

Dosage Forms ◽

Terbutaline Sulfate ◽

Liquid Chromatographic Method ◽

Silver Silver ◽

Silver Silver Chloride ◽

Liquid Chromatographic

Abstract A liquid chromatographic method with electrochemical detection has been developed for the determination of terbutaline sulfate in dosage forms. A cyanopropyl bonded-phase column is used with a mobile phase consisting of methanol-O.lM monobasic potassium phosphate containing 0.1M sodium heptanesulfonate and ImM disodium ethylenediaminetetraacetate (15 + 85). The compound of interest is detected at a glassy carbon electrode held at a potential of +0.9 V vs silver-silver chloride. The response is linear from 0 to 10 /«g/mL terbutaline sulfate. The method is applicable to tablet composites, individual tablets, dissolution determinations, and injections. Results and supporting data are reported for the above analyses.

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STUDY OF ACUTE TOXICITY OF A NEW VETERINARY DRUG FOR INTTRAMMARY INTRODUCTION

EUREKA Health Sciences ◽

10.21303/2504-5679.2018.00600 ◽

2018 ◽

Vol 2 ◽

pp. 51-60

Author(s):

Zhanna Polova

Keyword(s):

Acute Toxicity ◽

Lethal Dose ◽

Dosage Forms ◽

Veterinary Drug ◽

Test Substance ◽

Medicinal Products ◽

Preclinical Research ◽

Toxic Compounds ◽

White Rats ◽

Veterinary Medicinal Products

Preclinical studies of veterinary medicinal products are important and compulsory studies in the development of new dosage forms. The aim of preclinical research is to determine the toxic effect and therapeutic efficacy of the test substance-the future dosage form, its effect on the body's basic systems, as well as the identification of possible side effects. This work is part of the research on the development of the composition and technology of the veterinary drug - a solution for intramammary application, conventionally called "Argocide", intended for the treatment of mastitis in cattle. A study of the acute toxicity of the intramammary veterinary drug was carried out in experiments on white rats of both sexes, according to the requirements for potential medicines. The establishment of the value of the average lethal dose (LD50) of the veterinary drug "Argocide" with intramuscular single administration to white mature rats is impossible due to the absence of animal death even when the drug is administered at doses exceeding 5.0 ml/kg. This experiment allows the veterinary preparation "Argocide" to be classified as practically non-toxic compounds (V class). The analysis of the results of the conducted studies indicates the relative harmlessness of the potential drug for veterinary medicine and allows us to foresee that the "Argocide" preparation can be classified as low-risk substances, which justifies the expediency of its further study and introduction into practice.

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Prospective Nanotechnology-Based Strategies for Enhanced Intra- and Transdermal Delivery of Antifungal Drugs

Skin Pharmacology and Physiology ◽

10.1159/000511038 ◽

2020 ◽

Vol 33 (5) ◽

pp. 261-269

Author(s):

Ekaterina V. Lengert ◽

Ekaterina E. Talnikova ◽

Valery V. Tuchin ◽

Yulia I. Svenskaya

Keyword(s):

Fungal Infections ◽

Topical Therapy ◽

Local Treatment ◽

Hair Follicles ◽

Antifungal Drugs ◽

Prolonged Storage ◽

Future Improvement ◽

Systemic Side Effects ◽

Transdermal Penetration ◽

Storage Property

Topical therapy of superficial fungal infections allows the prevention of systemic side effects and provides drug targeting at the site of disease. However, an appropriate drug concentration in these sites should be provided to ensure the efficacy of such local treatment. The enhancement of intra- and transdermal penetration and accumulation of antifungal drugs is an important aspect here. The present overview is focused on novel nano-based formulations served to improve antimycotic penetration through the skin. Furthermore, it summarizes various approaches towards the stimulation of drug penetration through and into the stratum corneum and hair follicles, which are considered to be promising for the future improvement of superficial antifungal therapy as providing the drug localization and prolonged storage property at the targeted area.

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Plasma Biomarkers in Predicting Renal Recovery from Acute Kidney Injury in Critically Ill Patients

Blood Purification ◽

10.1159/000500423 ◽

2019 ◽

Vol 48 (3) ◽

pp. 253-261 ◽

Cited By ~ 1

Author(s):

Marco Fiorentino ◽

Fadi A. Tohme ◽

Raghavan Murugan ◽

John A. Kellum

Keyword(s):

Acute Kidney Injury ◽

Statistical Significance ◽

Kidney Injury ◽

Predictive Ability ◽

Renal Recovery ◽

Superior Performance ◽

Sensitivity Analyses ◽

Operating Characteristics ◽

Clinical Predictors ◽

Clinical Model

Background: Numerous studies have suggested a possible role for acute kidney injury (AKI) biomarkers in predicting renal recovery both before and after renal replacement therapy (RRT). However, definitions for recovery and whether to include patients dying but free of RRT may influence results. Objectives: To validate plasma neutrophil gelatinase-associated lipocalin (pNGAL) as a useful biomarker for predicting or improving the ability of clinical predictors alone to predict recovery following AKI, including in our model plasma B-type natriuretic peptide (pBNP) to account for cardiovascular events. Methods: We analyzed 69 patients enrolled in the Acute Renal Failure Trial Network study. pNGAL and pBNP were measured on days 2, 7, and 14. We analyzed their predictive ability for subsequent recovery, defined as alive and independent from dialysis in 60 days. In sensitivity analyses, we explored changes in results with alternative definitions of recovery. Results: Twenty-nine patients (42%) recovered from AKI. Neither pNGAL nor pBNP, alone or in combination, was accurate predictors of renal recovery-the best area under the receiver-operating characteristics curve (AUC) was for pNGAL using the largest relative change (AUC 0.59, 95% CI 0.45–0.74). The best clinical model achieved superior performance to biomarkers (AUC 0.69, 95% CI 0.56–0.81). The AUC was greatest (0.75, 95% CI 0.60–0.91) when pNGAL + pBNP on day 14 were added to the clinical model but this increase did not achieve statistical significance. However, integrated discrimination improvement analysis showed that the addition of pNGAL and pBNP on day 14 to the clinical model significantly improved the prediction of renal recovery (p = 0.008). Conclusions: pNGAL and pBNP can improve the accuracy of clinical parameters in predicting AKI recovery and a full model using biomarkers together with age achieved adequate discrimination.

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Tofacitinib Loaded Squalenyl Nanoparticles for Targeted Follicular Delivery in Inflammatory Skin Diseases

Pharmaceutics ◽

10.3390/pharmaceutics12121131 ◽

2020 ◽

Vol 12 (12) ◽

pp. 1131 ◽

Cited By ~ 1

Author(s):

Rebekka Christmann ◽

Duy-Khiet Ho ◽

Jenny Wilzopolski ◽

Sangeun Lee ◽

Marcus Koch ◽

...

Keyword(s):

Targeted Delivery ◽

Drug Exposure ◽

Skin Diseases ◽

Kinase Inhibitor ◽

Ex Vivo ◽

Topical Therapy ◽

Hair Follicles ◽

Janus Kinase ◽

Inflammatory Skin Diseases

Tofacitinib (TFB), a Janus kinase inhibitor, has shown excellent success off-label in treating various dermatological diseases, especially alopecia areata (AA). However, TFB’s safe and targeted delivery into hair follicles (HFs) is highly desirable due to its systemic adverse effects. Nanoparticles (NPs) can enhance targeted follicular drug delivery and minimize interfollicular permeation and thereby reduce systemic drug exposure. In this study, we report a facile method to assemble the stable and uniform 240 nm TFB loaded squalenyl derivative (SqD) nanoparticles (TFB SqD NPs) in aqueous solution, which allowed an excellent loading capacity (LC) of 20%. The SqD NPs showed an enhanced TFB delivery into HFs compared to the aqueous formulations of plain drug in an ex vivo pig ear model. Furthermore, the therapeutic efficacy of the TFB SqD NPs was studied in a mouse model of allergic dermatitis by ear swelling reduction and compared to TFB dissolved in a non-aqueous mixture of acetone and DMSO (7:1 v/v). Whereas such formulation would not be acceptable for use in the clinic, the TFB SqD NPs dispersed in water illustrated a better reduction in inflammatory effects than plain TFB’s aqueous formulation, implying both encouraging good in vivo efficacy and safety. These findings support the potential of TFB SqD NPs for developing a long-term topical therapy of AA.

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Alopecia: from clinic to preclinic and back

Pharmacy Formulas ◽

10.17816/phf18524 ◽

2019 ◽

Vol 1 (1) ◽

pp. 44-51

Author(s):

Dmitry Y. Ivkin ◽

Uliana V. Nogaeva ◽

Elena V. Flisyuk ◽

Marina V. Pisetskaya ◽

Yuri G. Shtyrlin

Keyword(s):

Animal Models ◽

Hair Loss ◽

Clinical Picture ◽

Rapid Growth ◽

Dosage Forms ◽

Hair Follicles ◽

Pharmaceutical Substances ◽

Phases Of Development ◽

Human Animal ◽

Personalized Approach

On average, 6070% of men and 2540% of women suffer from various forms of hair loss on our planet. If we turn to WHO statistics, we can see that about 75% of Russians are more or less susceptible to baldness. The hair follicle is an appendage of the skin, a kind of mini-organ that cyclically changes throughout a persons life. Periods of regeneration and rapid growth (anagen) alternate with periods of involution (catagen) and dormancy (telogen). As a rule, hair begins to fall out when the correlation between the number of hair follicles in different phases of development is violated. The occurrence of alopecia is associated with the influence of heterogeneous etiological factors, which further determine the pathogenesis of the disease and the clinical picture. The treatment of alopecia requires the use of a personalized approach to each patient. Both medicinal and cosmetic compositions are available for therapy in different dosage forms. At the same time, there remains a need for the search for new active pharmaceutical substances and the development of drugs based on them. However, in order to develop effective therapies, we need to reconstruct in detail the pathogenesis of alopecia on animal models. Then the extrapolation of the result human-animal-human will be accurate and problem-free, and the search for new means successful.

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Influence of Environmental Factors on the Primary Spontaneous Pneumotorax

Revista de Chimie ◽

10.37358/rc.18.10.6657 ◽

2018 ◽

Vol 69 (10) ◽

pp. 2937-2947

Author(s):

Tiberiu Lunguleac ◽

Marius Valeriu Hinganu ◽

Cristina Grigorescu ◽

Liviu Ciprian Gavril ◽

Paul Salahoru ◽

...

Keyword(s):

Environmental Factors ◽

Mechanism Of Action ◽

Seasonal Variability ◽

Spontaneous Pneumothorax ◽

Average Duration ◽

Statistical Significance ◽

Pleural Space ◽

Pleural Effusions ◽

Treatment Methods ◽

Duration Of Hospitalization

Pneumothorax is the presence of air between the two pleural effusions, making the pleural space from a virtual cavity to a real one. At present, we are facing a particular phenomenon: trying to establish with certainty the mechanisms underlying the occurrence of primary spontaneous pneumothorax and how to find and implement the best strategies for the application of treatment methods. Considering the classical conception that the incidence of spontaneous pneumothorax has a seasonal variability, we followed its distribution after the season, calendar month, by checking the statistical significance of the data obtained. Regardless of the dynamics factor involved and the likely mechanism of action, it seems to have an influence on the average duration of hospitalization and the length of time elapsed from intervention to discharge.

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