Study on the antioxidant activity during the formulation of biological active ingredient

Background& Aims:This study examined the antioxidant activity of different extract of parsley (Petroselinum crispum) with DPPH method. This assay is one of the most commonly used because of its simplicity and efficiency. Parsley is a widely known culinary plant and herbal medicine in Europe since ancient times. It is easy to grow and many biological activities are attributed to the flavonoids in the leaf. Biological active herbal medicines have an advantage over drugs because they are safer and cheaper. Methods: The antioxidant activities of the main flavonoid and its glycosides were measured. With previously optimized extraction procedure, the effect of particle size and extraction temperature were tested regarding the radical scavenging activity and drug content with spectrophotometric and HPLC-UV method. The antioxidant capacity of the extracts for 7 days were also investigated. Results: The aglicon possesses bigger antioxidant activity over the glycosidic forms. The scavenging activity was decreased with smaller the particle size of the dried leaves and higher temperature, but the flavonoid content was increased. Conclusion: The use of medicinal plants in the therapy is emerging. The exact dose and mode of action of the medicinal plants are still an unfolding area therefore the study on the main mode of action - the antioxidant activity – influenced by the formulation is important

Formulation and Characterization of Pulmonary Drug Delivery Systems

The inhalation therapy is one of the oldest drug delivery methods known. The significance of inhalation can be understood notably through its remarkable history. The goals of this review are to explore the pulmonary drug delivery, its significant relevance and various advantageous properties, particularly due to the physiology of the lungs. The drug delivery into the lungs can be provided by several inhalation instruments presently accessible on the market such as nebulizers, MDIs, and DPIs. Supplementary devices suchlike spacers for instance are also available in order to optimize the therapy results. The efficiency of these devices depends on several parameters of the formulation used, as well as its deposition in the lungs. Therefore, this review focuses on the meticulous testing performed on both the formulation and the device carrying it in the interest of insuring safety, quality, and efficacy of the final product. Ultimately, the pulmonary drug delivery represents a substantially advantageous alternative route of administration to obtain a systemic effect as well. This review aims to the better understanding of the development of pulmonary dosage forms and its complex process which requires extensive considerations and thorough optimization

Development of oral site-specific pellets containing flavonoid extract with antioxidant activity

Abstract Herbal medicines are recognized as an effective treatment of common diseases, mainly associated with oxidative stress. Therefore developing drug delivery systems of these biological active ingredients are gaining interest. Parsley (Petroselinum crispum L.) is a well-known culinary herb and its leaf contains high amount of apigenin, therefore it is suitable as a natural source of this flavonoid. Apigenin possess many health effects such as antioxidant, anti-inflammatory and anticancer activities. Unfortunately, these benefits are limited due to the low water solubility and bioavailability, it was recently classified as BCS II group compound. Therefore the aim of this study was to develop a carrier system for Petroselinum crispum extract, containing high amount of apigenin. Microcrystalline cellulose inert pellet cores were chosen and enteric coatings were applied. The produced multiparticulates had spherical shape, narrow size distribution and low moisture content. 10% (w/w) Eudragit® L 30 D-55 and 15% (w/w) Eudragit® FS 30 D coating was adequate for the modified release in vitro. The layered pellets demonstrated antioxidant activity. It was concluded that development of oral site-specific pellets containing flavonoid extract successful and the therapeutic effectiveness could be hypothesized

Optimization and Development of Albumin–Biopolymer Bioconjugates with Solubility-Improving Properties

Bioconjugation is an emerging field in the food and pharmaceutical industry. Due to its biocompatibility and high ligand binding capacity, albumin is widely used in modern drug delivery systems. However, the protein is sensitive to environmental stresses; albumin conjugates, on the other hand, have improved functional properties. Biopolymers are gaining interest due to their biodegradability and safety, compared to synthetic polymers. In this study, albumin–biopolymer bioconjugates were prepared by nonenzymatic Maillard reaction at 60 °C and 80% relative humidity. This nonenzymatic conjugation takes place between reducing sugars and available amino groups of a protein in certain conditions. The optimal molar ratio and time for the conjugation were studied by several investigation methods, including circular dichroism and fluorescence spectroscopy, sodium dodecyl sulfate–polyacrylamide gel electrophoresis (SDS–PAGE), and determination of available amino groups with ortho-phthaldialdehyde (OPA) assay. All of the measurements provided evidence for the covalent bonding of albumin and biopolymers, resulting in bioconjugates. Based on the results, a higher molar ratio and longer time are necessary to complete the reaction with the available amino groups. However, the optimal parameters are specific to each given biopolymer. The rheological behavior of the conjugates is characteristic of the initial biopolymer, which can be useful in drug development. Moreover, both the physical characteristics of albumin and the solubility-improving capacity were enhanced. Therefore, the potential use of albumin–biopolymer bioconjugates in the pharmaceutical industry could be considered

Rheological Considerations of Pharmaceutical Formulations: Focus on Viscoelasticity

Controlling rheological properties offers the opportunity to gain insight into the physical characteristics, structure, stability and drug release rate of formulations. To better understand the physical properties of hydrogels, not only rotational but also oscillatory experiments should be performed. Viscoelastic properties, including elastic and viscous properties, are measured using oscillatory rheology. The gel strength and elasticity of hydrogels are of great importance for pharmaceutical development as the application of viscoelastic preparations has considerably expanded in recent decades. Viscosupplementation, ophthalmic surgery and tissue engineering are just a few examples from the wide range of possible applications of viscoelastic hydrogels. Hyaluronic acid, alginate, gellan gum, pectin and chitosan are remarkable representatives of gelling agents that attract great attention applied in biomedical fields. This review provides a brief summary of rheological properties, highlighting the viscoelasticity of hydrogels with great potential in biomedicine

Comparative evaluation of the effect of cyclodextrins and pH on aqueous solubility of apigenin

Abstract The aqueous solubility of a flavonoid, apigenin, was studied in the presence of first generation cyclodextrins (α-CyD, β-CyD, γ-CyD), ionic and nonionic synthetic derivatives of β-CyD, namely SBE-β-CyD, HP-β-CyD and RM-β-CyD at various physiological pH. The order of solubility enhancement was as follows: RM-β-CyD > SBE-β-CyD > γ-CyD > HP-β-CyD > β-CyD > α-CyD. The phase solubility diagrams of HP-β-CyD and SBE-β-CyD indicated Higuchi AL subtype behavior, suggesting 1:1 stoichiometry of the complex. In contrast, AP subtype, so higher order complex formation can be assumed in the case of RM-β-CyD and γ-CyD. The formation of inclusion complexes has been confirmed by absorption and fluorescence spectroscopic measurements. Increased antioxidant activity was observed due to the inclusion complexes. These results prove that synthetic derivatives of β-CyD will be potentially useful excipients in the development of drug delivery systems for healthcare products containing flavonoids

Development and characterization of the voriconazole loaded lipid-based nanoparticles.

The number of topical fungal infections is growing, mostly owing to immunosuppressive therapy. Several topical fungal infections, such as eye mycoses, can be treated by local administration of antimycotic drugs. One major group of the antifungal agents is triazole, such as voriconazole (VCZ), which is used as the first line treatment of aspergillosis. A disadvantage of VCZ is its low water solubility making the drug difficult to administer in a liquid preparation. The lipid-based nanoparticles (LNP) have attracted increasing attention due to their advantageous properties. Contrarily to the conventional carrier systems, LNP can improve the poor solubility of topically used drugs, such as VCZ. Therefore, LNP represents promising alternatives to traditional carrier systems. The aim of the study was to formulate VCZ loaded lipid-based nanoparticles (VCZ-LNP) by high pressure homogenization (HPH). The developed LNPs were characterized by particle size analysis, IR spectroscopy, differential scanning calorimetry, dialysis test and antifungal efficacy studies. The particle size of the optimized nanoparticles from the selected lipid base, Witepsol(R) W35, was 182+/-4.1nm after five cycles of homogenization at 600bar. The antifungal study confirmed that the optimized VCZ-LNP inhibited the fungus reproduction