Claudia Clelia Assunta Juliano

Resveratrol inhibition of lipid peroxidation

To define the molecular mechanism(s) of resveratrol inhibition of lipid peroxidation we have utilized model systems that allow us to study the different reactions involved in this complex process. Resveratrol proved (a) to inhibit more efficiently than either Trolox or ascorbate the Fe2+ catalyzed lipid hydroperoxide-dependent peroxidation of sonicated phosphatidylcholine liposomes; (b) to be less effective than Trolox in inhibiting lipid peroxidation initiated by the water soluble AAPH peroxyl radicals; (c) when exogenously added to liposomes, to be more potent than α-tocopherol and Trolox, in the inhibition of peroxidation initiated by the lipid soluble AMVN peroxyl radicals; (d) when incorporated within liposomes, to be a less potent chain-breaking antioxidant than α-tocopherol; (e) to be a weaker antiradical than α-tocopherol in the reduction of the stable radical DPPH·. Resveratrol reduced Fe3+ but its reduction rate was much slower than that observed in the presence of either ascorbate or Trolox. However, at the concentration inhibiting iron catalyzed lipid peroxidation, resveratrol did not significantly reduce Fe3+, contrary to ascorbate. In their complex, our data indicate that resveratrol inhibits lipid peroxidation mainly by scavenging lipid peroxyl radicals within the membrane, like α-tocopherol. Although it is less effective, its capacity of spontaneously entering the lipid environment confers on it great antioxidant potential.

FORMULATION AND IN VIVO EVALUATION OF CHLORHEXIDINE BUCCAL TABLETS PREPARED USING DRUG-LOADED CHITOSAN MICROSPHERES

This investigation deals with the development of buccal formulations (tablets) based on chitosan microspheres containing chlorhexidine diacetate. The microparticles were prepared by a spray-drying technique, their morphological characteristics were studied by scanning electron microscopy and the in vitro release behaviour was investigated in pH 7.0 USP buffer. Chlorhexidine in the chitosan microspheres dissolves more quickly in vitro than does chlorhexidine powder. The anti-microbial activity of the microparticles was investigated as minimum inhibitory concentration, minimum bacterial concentration and killing time. The loading of chlorhexidine into chitosan is able to maintain or improve the anti-microbial activity of the drug. The improvement is particularly high against Candida albicans. This is important for a formulation whose potential use is against buccal infections. Drug-empty microparticles have an anti-microbial activity due to the polymer itself. Buccal tablets were prepared by direct compression of the microparticles with mannitol alone or with sodium alginate. After their in vivo administration the determination of chlorhexidine in saliva showed the capacity of these formulations to give a prolonged release of the drug in the buccal cavity.

Composition and in vitro antimicrobial activity of the essential oil of Thymus herba-barona Loisel growing wild in Sardinia

Abstract Two samples of the essential oils from Thymus herba-barona Loisel (Labiatae) of Sardinian origin were chemically characterized and their antimicrobial activity evaluated, in comparison with T. vulgaris and T. serpyllum oils, on the basis of their minimum inhibitory concentrations (M.I.C.s) and of the contact times required to totally inhibit development of microorganisms. GC and GC/MS analysis showed that the main components of essential oils of T. herba-barona were carvacrol (75.4% and 73–0%), borneol (3.6% and 6.4%) and p-cymene (3.9% and 3.3%), while the percentage of thymol was very low (1.0% and 0.7%). Results of the antimicrobial investigation demonstrated that both oils possessed similar and relevant microbicidal activities, especially against Gram+ bacteria (M.I.C.s range 0.125–0.500 mg/mL) and mycetes (M.I.C.s 0.125–0.500 mg/mL). At inhibitory concentrations, times required to kill microbial inocula (5–10 min) are comparable with those of chlorhexidine gluconate, an antiseptic with a broad range of antimicrobial activities. The strong activity of T. herba-barona oils is very probably due to the presence of carvacrol, which was found from our screenings to exhibit a similar antimicrobial activity. Our findings provide for a rationale basis of a possible utilization of this oil in fields requiring safe and cheap compounds with antiseptic and preservative properties, such as cosmetic, pharmaceutical and food industries.

Gold(I) complexes as antimicrobial agents

Seven gold complexes were prepared and investigated for biocidal activity against Gram-positive and -negative bacteria, fungi and protozoa. All of them were active against the tested microorganisms with the exception of Pseudomonas aeruginosa. In many, cases minimum inhibitory concentrations (MIC) were well below 1 microgram/ml. The activity is not simply related to the gold content, but also to the nature of both the phosphine and the aminothiol to which the metal is bound.

Mucoadhesive vaginal tablets as veterinary delivery system for the controlled release of an antimicrobial drug, acriflavine

The aim of the study was the development of mucoadhesive vaginal tablets designed for the local controlled release of acriflavine, an antimicrobial drug used as a model. The tablets were prepared using drug-loaded chitosan microspheres and additional excipients (methylcellulose, sodium alginate, sodium carboxymethylcellulose, or. Carbopol 974). The microspheres were prepared by a spray-drying method, using the drug to polymer weight ratios 1∶1 and 1∶2 and were characterized in terms of morphology, encapsulation efficiency, and in vitro release behavior, as MIC (Minimum Inhibitory Concentration), MBC (Minimum Bacterial Concentration), and killing time (KT). The tablets were prepared by direct compression, characterized by in vitro drug release and in vitro mucoadhesive tests. The microparticles have sizes of 4 to 12 μm; the mean encapsulation yields are about 90%. Acriflavine, encapsulated into the polymer, maintains its antibacterial activity; killing time of the encapsulated drug is similar to that of the free drug. In vitro release profiles of tablets show differences depending on the excipient used. In particular Carbopol 974, which is highly cross-linked, is able to determine a drug-controlled release from the matrix tablets for more than 8 hours. The in vitro adhesion tests, carried out on the same formulation, show a good adhesive behavior. The formulation containing microspheres with drug to polymer weight ratios of 1∶1 and Carbopol 974 is characterized by the best release behavior and shows good mucoadhesive properties. These preliminary data indicate that this formulation can be proposed as a mucoadhesive vaginal delivery system for the controlled release of acriflavine.

Spray-dried microspheres containing ketoprofen formulated into capsules and tablets

In this study, microspheres were prepared by a spray-drying technique using solutions of ketoprofen and two polymers, cellulose acetate butyrate (CAB) and hydroypropylmethylcellulose phthalate (HPMCP), in different weight ratios. Different total concentrations were used in the feed solutions: 3, 6 and 9% w/v. The spray-dried microparticles were characterized in terms of shape (SEM), size (light scattering method), production yield and encapsulation efficiency. They were formulated into capsules; tablets were prepared by direct compression of the microparticles mixed with maltose and, in some cases, hydroypropylmethylcellulose (HPMC). In vitro release studies were performed both at acidic and neutral pHs. The spray-drying process of solutions of ketoprofen with polymeric blends of cellulose derivatives leads to microparticles which, depending on their final formulation (capsules or tablets), can give a rapid or prolonged drug release. The formulations here described can be proposed for the oral administration of NSAIDs.In this study, microspheres were prepared by a spray-drying technique using solutions of ketoprofen and two polymers, cellulose acetate butyrate (CAB) and hydroypropylmethylcellulose phthalate (HPMCP), in different weight ratios. Different total concentrations were used in the feed solutions: 3, 6 and 9% w/v. The spray-dried microparticles were characterized in terms of shape (SEM), size (light scattering method), production yield and encapsulation efficiency. They were formulated into capsules; tablets were prepared by direct compression of the microparticles mixed with maltose and, in some cases, hydroypropylmethylcellulose (HPMC). In vitro release studies were performed both at acidic and neutral pHs. The spray-drying process of solutions of ketoprofen with polymeric blends of cellulose derivatives leads to microparticles which, depending on their final formulation (capsules or tablets), can give a rapid or prolonged drug release. The formulations here described can be proposed for the oral administration of NSAIDs.

Solid Lipid Microparticles (SLM) Containing Juniper Oil as Anti-Acne Topical Carriers: Preliminary Studies

Solid lipid microparticles (SLM) were used as carriers of juniper oil and proposed for the topical treatment of acne vulgare. The formulations were obtained by the o/w emulsification method. Compritol and Precirol were employed as lipidic materials. Emulsions containing 1.5% (w/w) of lipophilic phase (lipid and oil) and two different lipid to oil ratios (1:1 and 2:1) were prepared. Blank particles were also prepared, as a comparison. The SLM were characterized in terms of encapsulation efficiency, size, and morphology. The particle size stability in aqueous dispersions was monitored over one month. Evaporation of volatile compounds of oil from microparticles by weight loss was investigated. The qualitative composition of Juniper oil before and after the encapsulation process was determined by gas chromatography (GC) and gas chromatography/mass spectrum (GC/MS) analyses. The antimicrobial activity of the oil encapsulated into the lipid microparticles against P. acnes was studied as contact time assay and compared to the activity of the oil not encapsulated. The emulsification method here described was a good technique for the encapsulation of essential oils. Percentage yields of production and encapsulation efficiencies were higher for Compritol preparations than for these prepared using Precirol. All preparations were characterized by similar particle size distributions (dvs about 3–4 µm) regardless of lipid type and lipid to oil ratios. Microscopy observations showed that the microparticles in aqueous dispersions had almost spherical shape, independently from their composition. The scanning electron microscopy (SEM) analyses showed that when the particles were dried, they had an irregular shape and a rough surface. The SLM dispersions based on Compritol revealed particle size stability over the investigated period of 30 days. In contrast, an increase of the mean dimensions in the preparations containing Precirol was observed. A low loss of volatile oil compounds owing to evaporation from dry particles was found in all preparations. This indicated that the microparticles were able to substantially maintain the oil loaded inside their lipidic structure, reducing its volatility. Some modifications of composition were found in the oil encapsulated in SLM with respect to the juniper oil raw material, but these modifications did not decrease the antibacterial activity of the oil. The SLM here described are promising carriers for the development of anti-acne topical formulations containing Juniper oil.

Preparation and characterisation of polymeric films containing propolis

Propolis is a natural resinous substance, with a high polyphenol content, produced by honeybees and characterized by antimicrobial, anti-inflammatory and antioxidant properties, which make it useful for different therapeutic applications, especially in the stomatological field in the treatment of mild buccal diseases. The aim of this study was to prepare some polymeric film formulations for local delivery of propolis into the oral cavity. For this purpose, a commercial propolis fluid extract and three extracts (dry, ethanolic, glyceric) obtained from raw propolis were previously characterized with regard to their polyphenolic fraction composition and their antimicrobial properties against Candida albicans, Escherichia coli and Staphylococcus aureus strains. Commercial fluid extract, judged the most suitable in terms of polyphenol content and antimicrobial activity, was then incorporated into alginate, alginate-chitosan and agar films, prepared using a casting-solvent evaporation technique, which were finally evaluated in terms of thickness, total polyphenol content, in vitro polyphenol release profiles, swelling behaviour and antimicrobial properties. Our results demonstrate that polymeric films can be proposed as new propolis vehicles in the treatment of dental and buccal diseases.

In vitro antibacterial activity of antiseptics against vaginal lactobacilli

The results of investigations carried out to evaluate the inhibitory activity in vitro of seven vaginal antiseptic douche solutions against several strains of vaginal lactobacilli isolated from asymptomatic women are reported. Some of the products examined showed marked antibacterial activity even at high dilutions and for short exposure times. The post-antibiotic effect of two of these antiseptics on vaginal lactobacilli was also evaluated. The results of these investigations suggest that uncontrolled use of antiseptic products could cause changes in the normal vaginal flora.

Triorganotin compounds as antimicrobial agents

Six triorganotin derivatives of thiolupinine(1-mercaptolupinane), 2-mercaptobenzoxazole and 2-mercaptobenzothiazole were prepared and tested against several bacteria, fungi and protozoa. Most compounds exhibited high activity against the tested microorganisms and particularly worth noting was the activity of triethyltin lupinylsulfide on Gram-negative strains. Triethylgermanium lupinylsulfide was also prepared but was devoid of action on the whole set of tested microorganisms.