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1.
Colloids Surf B Biointerfaces ; 193: 111046, 2020 Sep.
Article in English | MEDLINE | ID: mdl-32416518

ABSTRACT

The purpose of this study was to develop miconazole nitrate (MN) based solid lipid nano-carrier formulae for topical delivery to enhance its antifungal effectiveness. Miconazole nitrate loaded Solid lipid nanoparticles (MN-SLNs) were formulated using a high shear homogenization technique characterized by particle size, polydispersity index (PI), trapping efficiency (EE percent), drug loading (DL percent) and zeta potential (ZP) characteristics. Furthermore, the optimized formulae were investigated for in-vitro release, ex-vivo study, skin toxicity test, and antifungal activity. With a particle size range of 244.2 ± 27.2 nm to 493.6 ± 35.3 nm, the selected MN-SLNs were spherical shaped. A high EE product percentage ranging from 79.38 ± 2.35 percent to 95.92 ± 6.12 percent and Zeta potential ZP values ranging from-21.6 ± 7.05 mV to-31.4 ± 6.84 mV suggesting strong stability was achieved. A controlled release of MN from the SLNs up to 48 h was shown in-vitro release study. The ex-vivo study showed that the selected MN-SLN (F4) mixture exhibited higher MN flux in the skin than a 1% MN solution. Moreover, selected MN-SLN (F4) has demonstrated a higher zone of inhibition against Candida albicans than a simple drug solution. MN-SLN (F4) had the lowest toxicity value for the skin. Besides, the MN-SLNs (F4) substantially reported antifungal activity with the least histopathological improvements compared to MN-solution utilizing immune-suppressing albino rats with induced candidiasis fungal infection. It can be fulfilled that SLNs can be acquired as a promising carrier for topical delivery of poorly soluble MN.


Subject(s)
Antifungal Agents , Azoles , Candida albicans , Lipids , Nanoparticles , Nitrates , Antifungal Agents/chemistry , Antifungal Agents/pharmacology , Azoles/chemistry , Azoles/pharmacology , Candida albicans/drug effects , Drug Carriers/chemistry , Drug Carriers/pharmacology , Drug Delivery Systems , Lipids/chemistry , Lipids/pharmacology , Microbial Sensitivity Tests , Nanoparticles/chemistry , Nitrates/chemistry , Nitrates/pharmacology , Particle Size , Surface Properties , Animals , Rats
2.
Article in English | MEDLINE | ID: mdl-30430947

ABSTRACT

INTRODUCTION: Betamethasone dipropionate is a highly effective corticosteroid anti-inflammatory. However, the main drawback of its topical use is the limited skin penetration into deeper skin layers. Also, its systemic use has shown many side effects. OBJECTIVE: The goal of this research was to formulate betamethasone dipropionate in nanostructured lipid carriers (NLC) formulae that contain oleic acid to aid its penetration to deeper skin layers and to aid absorption to local regions upon topical application. METHODS: NLC formulae were prepared by high shear homogenization then sonication. Formulae were characterized for their particle size, size distribution, electric potential, occlusion factor, entrapment efficiency, drug loading, transmission electron microscopy, in vitro drug release, and ex vivo skin penetration. Compatibility of ingredients with drug was tested using differential scanning calorimetry. Formulae were shown to have appropriate characteristics. NLC formulae were superior to traditional topical formulation in drug release. RESULTS: Upon testing ex vivo skin penetration, betamethasone dipropionate prepared in NLC formulae was shown to penetrate more efficiently into skin layers than when formulated as a traditional cream. NLC formulation that contained higher percentage of oleic acid showed higher penetration and higher amount of drug to pass through skin. CONCLUSION: In general, NLC with lower oleic acid percentage was shown to deliver betamethasone dipropionate more efficiently into deeper skin layers while that of a higher oleic acid percentage was shown to deliver the drug more efficiently into deeper skin layers and through the skin, transdermally.


Subject(s)
Betamethasone/analogs & derivatives , Drug Compounding/methods , Lipids/chemistry , Administration, Cutaneous , Animals , Betamethasone/administration & dosage , Betamethasone/chemical synthesis , Betamethasone/chemistry , Drug Carriers , Nanoparticles/chemistry , Particle Size , Skin/drug effects , Solubility , Surface-Active Agents/pharmacology , Transition Temperature
3.
AAPS PharmSciTech ; 17(3): 682-92, 2016 Jun.
Article in English | MEDLINE | ID: mdl-26314244

ABSTRACT

Antiadherents are used to decrease tackiness of a polymer coating during both processing and subsequent storage. Despite being a common excipient in coating formulae, antiadherents may affect mechanical properties of the coating film as well as drug release from film-coated tablets, but how could addition of antiadherents affect these properties and to what extent and is there a relation between the physical characteristics of the tablet coat and the drug release mechanisms? The aim of this study was to evaluate physical characteristics of films containing different amounts of the antiadherents talc, glyceryl monostearate, and PlasACRYL(TM) T20. Eudragit RL30D and Eudragit RS30D as sustained release polymers and Eudragit FS30D as a delayed release material were used. Polymer films were characterized by tensile testing, differential scanning calorimetry (DSC), microscopic examination, and water content as calculated from loss on drying. The effect of antiadherents on in vitro drug release for the model acetylsalicylic acid tablets coated with Eudragit FS30D was also determined. Increasing talc concentration was found to decrease the ability of the polymer films to resist mechanical stress. In contrast, glyceryl monostearate (GMS) and PlasACRYL produced more elastic films. Talc at concentrations higher than 25% caused negative effects, which make 25% concentration recommended to be used with acrylic polymers. All antiadherents delayed the drug release at all coating levels; hence, different tailoring of drug release may be achieved by adjusting antiadherent concentration with coating level.


Subject(s)
Acrylic Resins/pharmacokinetics , Drug Liberation , Polymers/pharmacokinetics , Polymethacrylic Acids/pharmacokinetics , Acrylic Resins/chemistry , Polymers/chemistry , Polymethacrylic Acids/chemistry
4.
Pharm Dev Technol ; 19(3): 304-14, 2014 May.
Article in English | MEDLINE | ID: mdl-23528038

ABSTRACT

OBJECTIVE: The aim of this study was to develop nanostructured lipid carriers (NLCs) as well as solid lipid nanoparticles (SLNs) and evaluate their potential in the topical delivery of meloxicam (MLX). MATERIALS AND METHODS: The effect of various compositional variations on their physicochemical properties was investigated. Furthermore, MLX-loaded lipid nanoparticles-based hydrogels were formulated and the gels were evaluated as vehicles for topical application. RESULTS AND DISCUSSION: The results showed that NLC and SLN dispersions had spherical shapes with an average size between 215 and 430 nm. High entrapment efficiency was obtained ranging from 61.94 to 90.38% with negatively charged zeta potential in the range of -19.1 to -25.7 mV. The release profiles of all formulations exhibited sustained release characteristics over 48 h and the release rates increased as the amount of liquid lipid in lipid core increased. Finally, Precirol NLC with 50% Miglyol® 812 and its corresponding SLN were incorporated in hydrogels. The gels showed adequate pH, non-Newtonian flow with shear-thinning behavior and controlled release profiles. The biological evaluation revealed that MLX-loaded NLC gel showed more pronounced effect compared to MLX-loaded SLN gel. CONCLUSION: It can be concluded that lipid nanoparticles represent promising particulate carriers for topical application.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Drug Carriers/chemistry , Lipids/chemistry , Nanoparticles/chemistry , Thiazines/administration & dosage , Thiazoles/administration & dosage , Administration, Cutaneous , Animals , Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics , Anti-Inflammatory Agents, Non-Steroidal/therapeutic use , Erythema/drug therapy , Erythema/pathology , Hydrogels/chemistry , Male , Meloxicam , Rats , Rats, Wistar , Skin/drug effects , Skin/metabolism , Skin/pathology , Skin Absorption , Thiazines/pharmacokinetics , Thiazines/therapeutic use , Thiazoles/pharmacokinetics , Thiazoles/therapeutic use
5.
Curr Drug Deliv ; 2(3): 289-94, 2005 Jul.
Article in English | MEDLINE | ID: mdl-16305431

ABSTRACT

The purpose of this study was to evaluate and compare the effect of glycerides with different fatty acid distributions (e.g. Arlacel 186, Capmul GMO and Captex 350) on Cyclosporine absorption in rat ileum segment using the modified single-pass intestinal perfusion with mesenteric vein cannulation. Drug concentration in the perfusate and blood plasma was analyzed by HPLC; and permeability coefficients were calculated from drug appearance in blood (P(blood)) and disappearance from perfusate (P(lumen)). Particle size was measured using Malvern Zetasaizer 1000HSA. Rheologic properties were measured using Brookfield viscometer. The results show that the average particle sizes after dilution (100 folds) of formulae containing Arlacel 186, Capmul GMO and Captex 350 and containing 0.8 mM CsA were 260+/-35.8, 130+/-11.4 and 37.5+/-6.0 nm, respectively. The polydispersity index was 0.6, 0.7 and 0.108 for formulations with Arlacel 186, Capmul GMO and Captex 350, respectively. CsA permeability coefficients (P(blood)) calculated from drug appearance in the blood in presence of Arlacel 186, Capmul GMO and Captex 350 were 0.3x10(-6), 1.0x10(-6) and 1.7x10(-6) cm2/sec, respectively. Phenol red was used as a water marker to determine net water absorption and secretion. Its constant concentration suggested that formulation did not alter intestinal water flux. From the results we can conclude that degree of glyceride esterification has a potential impact on the average particle size distribution and polydispersity of the formed micelles on dilution, which on turn contribute to the interaction between membrane and drug.


Subject(s)
Cyclosporine/pharmacokinetics , Glycerides/pharmacology , Immunosuppressive Agents/pharmacokinetics , Intestinal Absorption/drug effects , Mesenteric Veins/metabolism , Models, Animal , Animals , Male , Rats , Rats, Wistar
6.
AAPS PharmSciTech ; 5(4): e59, 2004 Jul 27.
Article in English | MEDLINE | ID: mdl-15760056

ABSTRACT

The purpose of this research was to evaluate beta-cyclodextrin (beta-CD) as a vehicle, either singly or in blends with lactose (spray-dried or monohydrate), for preparing a meloxicam tablet. Aqueous solubility of meloxicam in presence of beta-CD was investigated. The tablets were prepared by direct compression and wet granulation techniques. The powder blends and the granules were evaluated for angle of repose, bulk density, compressibility index, total porosity, and drug content. The tablets were subjected to thickness, diameter, weight variation test, drug content, hardness, friability, disintegration time, and in vitro dissolution studies. The effect of beta-CD on the bioavailability of meloxicam was also investigated in human volunteers using a balanced 2-way crossover study. Phase-solubility studies indicated an A(L)-type diagram with inclusion complex of 1:1 molar ratio. The powder blends and granules of all formulations showed satisfactory flow properties, compressibility, and drug content. All tablet formulations prepared by direct compression or wet granulation showed acceptable mechanical properties. The dissolution rate of meloxicam was significantly enhanced by inclusion of beta-CD in the formulations up to 30%. The mean pharmacokinetic parameters (C(max), K(e), and area under the curve [AUC](0-infinity)) were significantly increased in presence of beta-CD. These results suggest that beta-CD would facilitate the preparation of meloxicam tablets with acceptable mechanical properties using the direct compression technique as there is no important difference between tablets prepared by direct compression and those prepared by wet granulation. Also, beta-CD is particularly useful for improving the oral bioavailablity of meloxicam.


Subject(s)
Thiazines/chemistry , Thiazines/pharmacokinetics , Thiazoles/chemistry , Thiazoles/pharmacokinetics , beta-Cyclodextrins/chemistry , beta-Cyclodextrins/pharmacokinetics , Adult , Biological Availability , Chemistry, Pharmaceutical , Cross-Over Studies , Humans , Male , Mechanics , Meloxicam , Solubility , Tablets , Thiazines/blood , Thiazoles/blood , beta-Cyclodextrins/blood
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