Development of Microemulsion Dermal Products Based on Avocado Oil for Topical Administration

The research described in this study aimed at developing microemulsions for dermal application using avocado oil. Due to its composition, avocado oil helps maintaining the barrier function of the skin. It has a nutritional effect on the skin, and it reduces the intensity of the process of skin peeling. Various surfactant:cosurfactant systems were tested in the conducted studies. There were no significant differences between the diagrams generated by Tween 20 and the surfactant:cosurfactant system, Tween 20:PEG400, at a ratio of 1:1. Six formulations were selected from the dilution line 7 of the ternary phase diagrams obtained by using as a surfactant Tween 20 and Tween 20:PEG 400, respectively. The formulations were characterized by determining physicochemical properties specific. In the next phase of study, these six formulations were used as a vehicle for incorporating erythromycin in order to develop erythromicyn incorporated formulations for topical administration. The quality control of microemulsions with erythromycin was performed by evaluating the physical chemical, organoleptic and sensorial properties. Microemulsions were pharmacotechnically characterized by assessing the in vitro and ex vivo release kinetics of erythromycin

Effect of Apitherapy Formulations against Carbon Tetrachloride-Induced Toxicity in Wistar Rats after Three Weeks of Treatment

The human body is exposed nowadays to increasing attacks by toxic compounds in polluted air, industrially processed foods, alcohol and drug consumption that increase liver toxicity, leading to more and more severe cases of hepatic disorders. The present paper aims to evaluate the influence of the apitherapy diet in Wistar rats with carbon tetrachloride-induced hepatotoxicity, by analyzing the biochemical determinations (enzymatic, lipid and protein profiles, coagulation parameters, minerals, blood count parameters, bilirubin levels) and histopathological changes at the level of liver, spleen and pancreas. The experiment was carried out on six groups of male Wistar rats. Hepatic lesions were induced by intraperitoneal injection of carbon tetrachloride (dissolved in paraffin oil, 10% solution). Two mL per 100 g were administered, every 2 days, for 2 weeks. Hepatoprotection was achieved with two apitherapy diet formulations containing honey, pollen, propolis, Apilarnil, with/without royal jelly. Biochemical results reveal that the two apitherapy diet formulations have a positive effect on improving the enzymatic, lipid, and protein profiles, coagulation, mineral and blood count parameters and bilirubin levels. The histopathological results demonstrate the benefits of the two apitherapy diet formulations on reducing toxicity at the level of liver, spleen and pancreas in laboratory animals

FORMULATION AND PREPARATION OF ORALLY DISINTEGRATING TABLETS USING INNOVATIVE BINDER

Abstract The present study investigates the use of glyceryl palmitostearate (Precirol ATO 5 -coded PATO) as binder in orally disintegrating tablets (ODT), prepared by melt granulation. PATO has been mentioned in literature for its lipophilic nature and fine powder properties, providing excelent coating and slow release of active drugs, but it can also be used for taste masking purposes, with possible applications in ODT. In order to use it as an ODT excipient, some challenges must be overcome, given its lipophilicity. Our first goal was to study its potential to improve tablet properties (hardness, friability, disintegration time) and provide fast release of the model drug, by setting the optimal proportion to be used in ODT. We investigated a complete 3 3 experimental design with 9 formulations containing 300 mg acetaminophen; the independent variables were: proportion of PATO binder (2.5-7.5 %) and proportion of sodium starch glycolate (Explotab) as superdisintegrant (5-10 %). The regression equations and response surface plots showed the validity of the model, and a significant influence of PATO on the response variables: tablet hardness, disintegration time, and active drug release in a short time. We can conclude that Precirol ATO 5 can be used as binder in ODT (not more than 5 %), higher proportions having a slow-release effect. Also, together with 8 % disintegrant, it provides good tablet properties, fast disintegration and a release of 80 % acetaminophen after 10 min. Rezumat Studiul investighează utilizarea excipientului glicerol palmitostearat (Precirol ATO 5-PATO) ca liant în comprimatele orodispersabile (ODT) preparate prin metoda melt granulation. PATO are proprietăţi lipofile accentuate şi o fineţe avansată a pulberii, fiind recomandat în literatură ca agent de acoperire, dar şi de retardare în comprimate; el poate fi utilizat şi ca agent de mascare a gustului, aplicaţie utilă în formularea ODT. Utilizarea lui în ODT trebuie să depăşească inconvenientele legate de lipofilia sa, păstrând calităţile care pot fi utile în acest tip de formulare: îmbunătăţirea proprietăţilor comprimatelor (duritate, friabilitate, timp de dezagregare) şi o cedare accelerată a substanţelor active, prin stabilirea unei proporţii optime de PATO care să asigure calităţile menţionate. Ca substanţă-model s-a ales paracetamolul (300 mg/comprimat) şi s-a construit un plan experimental complet 3 3 cu 9 experimente, în care variabilele independente au fost proporţile de PATO (2,5-7,5 %) şi amidon glicolat de sodiu ca dezagregant (5-10 %). Ecuaţiile de regresie şi suprafeţele de răspuns au confirmat validitatea modelului ales, liantul PATO influenţând proprietăţile FARMACIA, 2013, Vol. 61, 6 1132 comprimatelor, dar şi cedarea paracetamolului. Putem concluziona că liantul Precirol ATO 5 este util în ODT în proporţia maximă de 5 %, peste această limită manifestând un efect de încetinire a cedării. Asociat cu 8 % dezagregant asigură proprietăţi corespunzătoare pentru ODT şi o cedare a paracetamolului de 80 % după 10 minute

Controlling the release kinetics of calcein loaded liposomes from chitosan/tannic acid and chitosan/poly(vinyl alcohol)/tannic acid hydrogels

International audienceThe paper describes the preparation of novel hydrogels based on chitosan or chitosan/poly(vinyl alcohol) crosslinked with tannic acid for the inclusion of phosphatidylcholine liposomes loaded with calcein as model fluorescent hydrophilic drug. This procedure ensured the reduction of the “burst effect” or even its elimination. The originality of the paper consists in the utilization of the natural compound tannic acid as crosslinker for the formation of complex hydrogels, which ensures biocompatibility and excellent biological properties. In order to modulate the properties of the hydrogel, the molecular weight of chitosan, the chitosan/tannic acid molar ratio, the molar ratio between the polymers and the crosslinking time have been taken into account as variable parameters. Hydrogels based on medium molecular weight showed a reduced degree of swelling, as compared to those containing high molecular weight chitosan. More tannic acid in the hydrogel composition resulted in a higher crosslinking density in the hydrogels and reduced the swelling degree. As it was expected, the use of the synthetic polymer reduced the hydrophilicity of the materials and, as a consequence, the drug release capacity. Surprisingly, the crosslinking time did not reduce significantly the maximum degree of swelling. In good correlation with the characteristics of the hydrogels, the calcein release from the complex hydrogels could be delayed and better controlled. The release time was prolonged from several days (control hydrogels) to 21 days. The latency parameter showed that more that 40% of the calcein was released in the form of liposomes, which constitutes a second release barrier for the included drug

Development of a Prolonged-Release Drug Delivery System with Magnolol Loaded in Amino-Functionalized Mesoporous Silica

Magnolol (MG) is a small-molecule neolignan polyphenolic compound isolated from the genus Magnolia. The anti-inflammatory, anti-oxidative, anti-diabetic, anti-tumorgenic, anti-neurodegenerative, anti-depressant and anti-microbial properties of MG are well documented in recent literature. These fascinating multiple biological activities of MG encourage research about the development of new delivery and administration approaches able to maximize its potential benefits. This study describes the amino-functionalization of the SBA-15 (Santa Barbara Amorphous) mesoporous matrix by post-synthesis grafting using APTES (3-aminopropyltriethoxysilane) and the characterization of amino-functionalized mesoporous silica SBA-15 loaded with MG in order to achieve modified drug delivery systems. The amino-functionalization of silica SBA-15 was carried out by grafting by refluxing in dry toluene. The powders obtained were characterized texturally by Brunauer-Emmett-Teller (BET) surface area analysis measurements and morphologically by scanning electron microscopy. MG loading degree in the nanoporous matrix was determined by the HPLC method at λ = 290 nm. Results showed that by grafting the amino groups in the silica SBA-15, we obtained amino-functionalized silica SBA-15 with an ordered structure, with specific surfaces and pore sizes that differ from the original matrix, which was reflected in the amount of MG immobilized and release kinetics profile

“Off-Label” use of antibiotics in critical patients

In intensive care units, the most prescribed drugs are antibiotics, as result of the high incidence of infections among patients admitted to these units. In medical practice, antibiotic resistance is a phenomenon with dramatic consequences, which has led to the development of new strategies to solve this public health problem, including the use of ”off-label” drugs. Classification as an off-label prescription of a drug mainly refers to: unapproved therapeutic indication, formulation, dose (including dose interval), age or unapproved route of administration. The aim of this paper is to present the categories of appropriate ”off-label” use of drugs with a detailed description of the principles of use in this regime of antibiotics as mono- or combo-therapy