Kaolin in pharmaceutical preparations: a review

Background: Kaolin is a clay mineral with Al2Si2O5(OH)4 structure which can be found in sedimentary rocks also known as clay stones. Kaolin consists of clay materials such as quartz, illite, smectite, and hematite, with the largest constituent component being kaolinite. Kaolin is one of the most common minerals with an abundant presence in the earth's crust compared to other minerals, especially in Indonesia. In the pharmaceutical sector, this clay mineral is widely used in Indonesia. Kaolin is known to be a good adsorbent and has good physical, chemical, and surface physicochemical properties. Objective: This review article aims to provide information about the uses of kaolin in the pharmaceutical industry. Methods: This review article was written by conducting a literature search study method in the PubMed, ScienceDirect, and Google Scholar databases. Results: In the pharmaceutical field, kaolin is used as an excipient in various types of medicinal preparations, one of which is as a suspension agent because of its ability to stabilize suspensions in a deflocculated state as an emulsifying agent, crushing agent, filling agent, and drug carrier. As an active substance, kaolin is widely used because it has a therapeutic activity. In the cosmetic industry, kaolin can be administered in a variety of topical dosage forms which act as skin protective agents or sunscreens. Conclusion: Based on the results of the review, it was found that kaolin, with its abundant presence on earth and its great potential in the pharmaceutical field, is used as an active medicinal substance, excipient ingredient, and in the cosmetic field as a sunscreen. Keywords: Kaolin, excipient, active pharmaceutical ingredient, cosmetics

3D-Printed Products for Topical Skin Applications: From Personalized Dressings to Drug Delivery

3D printing has been widely used for the personalization of therapies and on-demand production of complex pharmaceutical forms. Recently, 3D printing has been explored as a tool for the development of topical dosage forms and wound dressings. Thus, this review aims to present advances related to the use of 3D printing for the development of pharmaceutical and biomedical products for topical skin applications, covering plain dressing and products for the delivery of active ingredients to the skin. Based on the data acquired, the important growth in the number of publications over the last years confirms its interest. The semisolid extrusion technique has been the most reported one, probably because it allows the use of a broad range of polymers, creating the most diverse therapeutic approaches. 3D printing has been an excellent field for customizing dressings, according to individual needs. Studies discussed here imply the use of metals, nanoparticles, drugs, natural compounds and proteins and peptides for the treatment of wound healing, acne, pain relief, and anti-wrinkle, among others. The confluence of 3D printing and topical applications has undeniable advantages, and we would like to encourage the research groups to explore this field to improve the patient’s life quality, adherence and treatment efficacy.

PHYSICAL STABILITY TEST AND ETHANOL CREAM IRRITATION TEST OF Moringa oleifera L.

The development of topical dosage forms of Moringa leaf extract cream has been carried out because of its properties that can moisturize the skin. A pharamceutical preparation must meet the requirements of stability and non toxic. The study aimed to determine the effect of variations un the concentration ethanol extract cream of Moringa leaf of physical stability and irritability. Ethanol extract of Moringa leaves was obtained by maceration method with 50% ethanol solvent. The extract was then formulated in the form of O/W base scarring with concentrations of 1% (F1), 3% (F2), and 5% (F3). Creams were evaluated for physical stability including mechanical tests (centrifugation) and physical stability at room temperature (25 ± 2oC) with parameters pH, viscosity on days 1, 7, 14, 21 and 28. In addition, creams were also evaluated for their irritability in vivo with using test animals (rabbits). The data obtained were analyzed using one-way ANOVA test. The results of the physical stability test showed that an increase in the concentration of Moringa leaf extract caused an increase in viscosity (P <0.5) and a decrease in pH (P <0.5) but did not affect physical stability (mechanical test) and its irritating effect. F2 (1%) has a pH of 7.61 while F4 (5%) is 7.01. Based on the results of the study, it is concluded that variations in the concentration of ethanol extract of Moringa leaves can affect the physical stability of the cream and do not affect its irritation properties. Moringa leaf ethanol extract cream with a concentration of 5% (F4) has physical stability and does not irritate the skin better than other formulas.

Adherence to treatment in patients with inflammatory bowel disease

Inflammatory bowel disease (IBD) is a common pathology that reduces the quality and duration of a patient’s life. The cornerstone of treatment of IBD patients is polypharmacotherapy based on the use of salicylates, antibiotics, immunomodulatory and biological drugs, and topical dosage forms. Multicomponent treatment has shown to reduce the quality of life and negatively affect adherence to drug therapy in IBD patients.One of the leading causes of treatment failure is low treatment adherence, which leads to disease progression, disability, and increased financial costs. Currently, there are many factors that affect adherence to therapy, some of them are modifiable, which creates opportunities to improve the effectiveness of existing medical interventions. However, the available data on the level of adherence in IBD patients are not numerous and homogeneous, so a low level of adherence to drug therapy in IBD patients is registered in 7–72% of cases.An important issue in understanding adherence in IBD patients is a lack of research on the level of adherence to counselling and lifestyle modification. However, the course of IBD, treatment features related to the duration of therapy and necessary lifestyle modifications (nutrition), as well as regular monitoring of laboratory and instrumental parameters determine the need to assess adherence to lifestyle modification and counselling along with adherence to drug therapy.

Solubility and Partition Coefficient of Salicylamide in Various pH Buffer Solutions

The solubility and partition coefficient are essential physicochemical parameters in developing a pharmaceutical dosage form of medicine. In addition, these parameters help to predict the absorption of an active compound in oral or topical dosage forms. Salicylamide, an active ingredient available in oral and topical dosage forms, is a weak acid (pKa 8.2) and is sparingly soluble in water. Meanwhile, its solubility and partition coefficients are influenced by the pH of the environment. The Henderson-Hasselbalch equation is used to predict solubility-pH and partition-pH profiles at various pH solutions. This study aims to determine salicylamide's solubility and partition coefficient in various pH (2–11). Both tests were carried out in various pH buffer solutions (at a concentration of 0.02 M and 0.2 ionic strength) in a water bath shaker at a temperature of 37 ± 0.5 °C. In addition, the salicylamide content was determined using the UV spectrophotometer method at the maximum wavelength at each pH. The results showed that the solubility increased at pH 2–10, while the partition coefficient value decreased. On the other hand, at pH 11, there was an increase in the number of ionized species, but the solubility decreased.

Preparation of Azithromycin Nanofibers as Controlled Release Ophthalmic Drug Carriers Using Electrospinning Technique: In-Vitro and in-Vivo Characterization

Purpose: Conventional topical dosage forms face with some challenges like low intraocular bioavailability, which could be overcome by application of novel drug delivery systems. Therefore, this study was conducted to prepare azithromycin (AZM)-loaded chitosan/polyvinyl alcohol/polyvinyl pyrrolidone (CS/PVA-PVP) nanofibers with the prolonged antibacterial activity by electrospinning method. Methods: After preparation of nanofibers, they were characterized in terms of physicochemical and morphological properties. In-vitro and in –vivo release of the drug from nanofibers were evaluated using microbial assay against the Micrococcus luteus. Antibacterial efficacy of the nanofibers was assessed. The ophthalmic irritation test was also performed. MTT test was carried out to evaluate cytotoxicity of the formulations. Results: All the formulations were found to be stable with uniform thickness, weight, and drug content. Nanofibers had a diameter range from 119±29 to 171±39 nm. The inserts were non-irritant and non-toxic to the rabbits҆ eye. Based on the obtained results, the crosslinked AZM nanofibers showed slower and more controlled drug release in tear fluid compared to the non-crosslinked ones, within 184 h. Conclusion: Our results revealed that the prepared nanofibers could be considered as suitable and non-invasive inserts for the prolonged ophthalmic delivery of azithromycin.

Recent advancement in topical drug delivery for psoriasis: Clinical Pertinence and Potential Market

: Psoriasis is an immune-mediated chronic skin inflammation. This disease can be associated with several manifestation like red flaks, silver scale, patches, plaques and silvery-white squams. Approximately 70% of the patients treated with topical dosage forms have a mild-to-moderate form of psoriasis, whereas a moderate-to-severe form of psoriasis is treated with systemic, photo, and biological therapies. Considering the big fraction that topicals cover, we present the current market potential, clinical relevance, and recent advances in the topical delivery of the drug for psoriasis. Though we witnessed several advancements in the recent few decades, delivering new immunomodulatory and biological molecules for topical psoriatic treatment have been proved efficient and safe option for the large percentage of patients for whom systemic therapy is not indicated. This article enumerates the promising topical dosage forms at present under assessment for their clinical pertinence. The competency of conventional topicals to reach and transform the world market is enumerated in terms of their success rate after proving the clinical pertinence against psoriasis. However, the entrance of novel drug delivery systems based advanced topical products in the global market is highly anticipated as they have immense potential to precedent tremendous impact on psoriasis treatment in near future.

Topical application of Apremilast in the treatment of mild to moderate psoriasis

Mild to moderate psoriasis is highly prevalent in about 80% of the global psoriatic population. Current available treatment options for mild to moderate psoriasis are topical dosage forms and are associated variety of setbacks. To address these setbacks, Apremilast topical gels, 2% & 4%, w/w were developed, and a clinical proof of concept study (POC) was performed to establish efficacy and safety. A single centre randomized, double-blind, placebo-controlled study was conducted with apremilast topical gels 2% & 4% w/w in adult mild to moderate psoriatic patients for 12 weeks. The efficacy of the gels was evaluated by comparing the PASI scores before and after treatment of 12 weeks. Both gels exhibited a significant reduction in PASI values when compared with baseline PASI scores. An average percentage inhibition of PASI with test products, i.e. 2% and 4% w/w Apremilast topical gels, are about 46.8% and 34.6%, respectively, after 12 weeks of treatment. The results confirm that the apremilast topical gels are a good option for the treatment of mild to moderate psoriasis and have to be explored further.

FORMULASI EMULGEL DARI EKSTRAK DAUN KELOR (Moringa oleifera LAM) SERTA EVALUASI AKTIVITAS ANTIOKSIDAN DENGAN METODE DPPH

Moringa (Moringa oleifera Lam) is one of the plants that has high antioxidant activity, especially in the leaves. Emulgel is one of the topical dosage which dermatologically has several beneficial properties, namely thixotropic, not oily, easy to spread, easy to clean, soft, easy to wash, long lasting, transparent and comfortable when used. The purpose of this research was to formulate moringa (Moringa oleifera Lam) leaves extract into emulgel dosage forms and determine the antioxidant activity of the dosage using DPPH method.The research began with extraction of moringa leaves and optimization of the base by varying the concentration of carbopol 940 as gelling consisting of F1 0.5%, F2 1%, F3 1.5% and F4 2%. The base that met the requirements of good physical stability was F2. The F2 base was then made into emulgel dosage with 3 concentration variations of the extract, namely F2a 4%, F2b 5% and F2c 6%. The physical stability test result of each formula met the organoleptic test,the pH test, the dispersion test, the adhesion test, the viscosity test, and the freeze-thaw test. The One way ANOVA statistical test result showed that the p value was greater than 0.05, which meant that the emulgel dosage had good physical stability. The IC50values of each antioxidant activity result were F2a (t0 = 120.464 g/mL; t28 = 144.887 g/mL), F2b (t0 = 113.642 g/mL; t28 = 128.407g/mL), F2c (t0 = 74.745 g/mL; t28 = 90.618 g/mL). The statistical results of the t-test showed thep value = 0,027, (0.05), This indicated that there were significant difference results of the antioxidant activity test between the three formulas on the first day (t0) and on the 28th day (t28).