Final Formulation Research Articles

Safety Assessment of Butyrospermum parkii (Shea)-Derived Ingredients as Used in Cosmetics.

The Expert Panel for Cosmetic Ingredient Safety (Panel) assessed the safety of 13 Butyrospermum parkii (shea)-derived ingredients, which are most frequently reported to function in cosmetics as skin and hair conditioning agents. The Panel reviewed the available data to determine the safety of these ingredients. Because final product formulations may contain multiple botanicals, each containing similar constituents of concern, formulators are advised to be aware of these constituents and to avoid reaching levels that may be hazardous to consumers. Industry should use good manufacturing practices to limit impurities that could be present in botanical ingredients. The Panel concluded that these ingredients are safe in the present practices of use and concentration when formulated to be non-sensitizing.

Brašno i izolati proteina boba kao delimični supstituenti u hlebu od mešavine pšenice i tritikalea - tehnološka i senorska svojstva

The incorporation of faba bean flour (FBF) and protein isolate (FBI) into wheat-triticale flour blends is a potential promising strategy to enhance the nutritional and functional properties of bread. This study aimed to investigate the potential of these ingredients from both technological and sensory perspectives. Multiple analyses were conducted, including chemical composition, texture profile analysis, colour, specific volume and sensory properties of breads made with a blend of wheat and triticale flours (70:30). Part of the blend was substituted with either 20% faba bean flour or 7.2% faba bean protein isolate to ensure an equal proportion of faba bean protein in the final formulations. The results showed a significant increase in protein content for both FBF and FBPI breads, with the faba bean protein isolate also increasing the ash content. Texture profile analysis (TPA) indicated that the substitutions affected bread properties by increasing hardness, gumminess, and chewiness, particularly in bread with FBI. However, cohesiveness, springiness, and resilience decreased similarly in both cases. Additionally, the specific volume decreased with the addition of faba bean flour and protein, especially in FBI bread. From the colour aspect, analysis revealed a darker hue and a more pronounced reddish nuance in the bread crust in FBF and FBI breads. Sensory evaluation indicated a slightly lower overall likeability with faba bean addition, yet the breads remained acceptable to the panellists. Detailed sensory analysis supported the TPA findings and colour differentiation, showing higher values for hardness, crust compactness, and crumbliness. Texture and colour were rated lower compared to the control sample. Moreover, both FBF and FBI breads exhibited higher overall odour intensity. Specifically, bread with the protein isolate had less uniform pores and a more pronounced flour/cereal/bran odour. In contrast, bread with faba bean flour had more uniform pores but a noticeable bitterness. In conclusion, this study demonstrates that faba bean flour and protein isolate can be used as partial substitutes in wheat-triticale flour blends to produce bread with acceptable properties. This leaves room for future in-depth analysis and modifications to address the identified challenges.

Formulation and Validation of An Analytical Method for the Estimation of Rabeprazole Sodium Delayed-Release Tablets

Background Rabeprazole sodium is a proton pump inhibitor used for the treatment of peptic ulcer and gastroesophageal reflux disease by inhibiting the enzyme HKATPase the acidic pump. In addition erosive esophagitis and Zollinger-Ellison syndrome are treated with it.In this study the objective was to develop a pharmaceutically stable and cost-effective and quality-improved formulation and UV spectrophotometry method have been developed to estimate Rabeprazole sodium delayed-release tablets. To achieve these goals various prototype formulation trails will be taken and evaluated.Methods Rabeprazole sodium prolonged release tablets were prepared by direct compression technique used to the different excipients as well as varying concentrations of polymer proportion using HPMC phthalate 55 which is an enteric coating material.Results The results indicated that the final product formulation 12 met all the specifications of the physical properties and invitation release and is comparable to the innovator product.Conclusions In the present study Rabeprazole enteric-coated tablets were prepared using HPMC phthalate 55 enteric polymer. Formulation 12 was found to be the best of all formulations showing drug release that matches the innovator product so all quality control tests were performed for conformation for the formulation. The tablets were tested for acid release during the stability period and the results confirmed that the results were within the limits.

The colorful fungi of the Chilean forests: Production, chemical characterization and possible applications of their pigments.

In Chile, as in the rest of the world, only a small fraction of the fungal diversity inhabiting the wide variety of its ecosystems is known. This diversity must hide an inestimable richness of species with interesting biotechnological potential, including fungal pigment producers. Recently, interest in filamentous fungi has increased significantly due to their importance as alternative sources of pigments and colorants that are environmentally and human health friendly. As a result, fungal pigments are gaining importance in various industrial applications, such as food, textiles, pharmaceuticals, cosmetics, etc. The increasing consumer demand for "green label" natural colorants requires the exploration of different ecosystems in search of new fungal species that are efficient producers of different pigment with a wide range of colors and ideally without the co-production of mycotoxins. However, advances are also needed in pigment production processes through fermentation, scale-up from laboratory to industrial scale, and final product formulation and marketing. In this respect, the journey is still full of challenges for scientists and entrepreneurs. This chapter describes studies on pigment-producing fungi collected in the forests of central-southern Chile. Aspects such as the exploration of potential candidates as sources of extracellular pigments, the optimization of pigment production by submerged fermentation, methods of pigment extraction and purification for subsequent chemical characterization, and formulation (by microencapsulation) for potential cosmetic applications are highlighted. This potential use is due to the outstanding bioactivity of most fungal pigments, making them interesting functional ingredients for many applications. Finally, the use of fungal pigments for textile and spalting applications is discussed.

Liposomal factor VIII as an efficient pharmaceutical system for the treatment of hemophilia.

Currently, the most important treatment approach for hemophilia type A is recombinant Factor VIII. However, due to its low retention time in the blood, the patients usually need successive injections. In addition, neutralization of injected proteins by antibodies complicates treatment. We examined the prolongation of the persistence time of injectable FVIII in the blood and the potential effects on survival using promising PEGylated liposomes (PEGLip) utilizing hydrogenated soy phosphatidylcholine (HSPC, Tm= 54.5 ºC) and 1-palmitoyl-2-oleoyl-phosphatidylcholine (POPC, Tm= - 2 ºC). Nanoliposomes with different percentages of PEG (3% and 5%) were obtained via the thin film hydration procedure and extrusion. Liposomal FVIII formulation was prepared and characterization was done. The results revealed that the formulations are in the 80-120 nm range with uniform dispersion, which was confirmed using transmission electron microscopy (TEM) imaging. The phase transition temperature (Tm) of the liposomes was obtained by differential scanning calorimetry (DSC). With an attachment efficacy of approximately 87%, proteins bind non-covalently yet with a strong affinity to the exterior of PEGLip. The final formulations underwent additional examination. No significant change was observed in size, charge, and PDI between the FVIII-conjugated liposomal formulations and their liposomal nanoparticles. The selected formulations were injected into BALB/c mice. The circulation time and potential clotting effectiveness of PEGLip-FVIII are vastly improved over free protein, in non-hemophilic mice. The obtained results showed that using phospholipids with high Tm (HSPC) can improve the hemostatic efficiency of liposomes more than phospholipids with low Tm (POPC).

Box-Behnken guided development of an ecofriendly RP-HPLC analytical method for simultaneous quantification of pantoprazole sodium and piperine co-loaded mucoadhesive GRDDS formulation for H. pylori eradication

Helicobacter pylori (H. pylori) infection is the leading cause of chronic peptic ulcer disease worldwide. Many treatment options are available to treat H. pylori infection. However, the eradication is still a challenge due to the poor bioavailability of the currently available formulations. To improve the efficacy of therapy, novel formulations are necessary. Proton pump inhibitors (PPIs) are already a part of the treatment regimen with antibiotics. P-glycoprotein (P-gp) inhibitor was reported to have increased the efficacy of antibiotic treatment in H. pylori infections. To make available the P-gp inhibitor and PPI on the intestinal mucosal surface we have formulated a gastroretentive drug delivery system (GRDDS) as an adjuvant therapy with antibiotics. The objective of this study is to simultaneously estimate pantoprazole (PAN) and piperine (PIP) by reverse-phase (RP) high-performance liquid chromatography (HPLC) method from the chitosan-based sodium alginate mucoadhesive beads utilizing the design of experiments (DOEs) methodology. The HPLC settings were optimized using DOEs software. The final optimized HPLC method used a hyperclone Octadecylsilane C18 column as the stationary phase and methanol: ammonium acetate at pH 4.5 (70:30 v/v) as the mobile phase. The flow rate was 0.9 ml/minute. The validation of the developed RP-HPLC method was done as per the International Conference on Harmonization (ICH) Q2(R1) guideline. The method was linear from 0.5 to 20 μg/ml for both PAN and PIP with an R2 value of 0.999 and 0.999, respectively. The validated RP-HPLC method showed specificity for both drugs despite interference from degradation products and other GRDDS excipients. The entrapment efficiency of the final formulation was determined to be 80%–85% for PAN and 60%–67% for PIP. The novelty and merit of the DOE-based method development are that it reduces the number of trials, thereby reducing reagent wastage, and is environmentally friendly suggested by the Green Analytical Procedure Index (GAPI) tool scoring six green, six yellow, and three red.

Development of flavored kombuchas with Amazonian fruits: bioactive compounds evaluation and antioxidant capacity.

Using Amazonian fruits to flavor kombuchas is a promising proposal, as it adds nutritional value to the drink. This work sought to develop kombucha flavored with Amazonian fruits and evaluate the bioactive compounds and antioxidant capacity of the formulations. Three kombucha formulations were prepared using green tea (Camellia sinensis) and three Amazonian fruits: cupuassu (Theobroma grandiflorum), tapereba (Spondias lutea L.) and bacuri (Platonia insignis). Kombucha fermentations were evaluated before and after the insertion of nectars through the analysis of phenolic compounds, vitamin C and antioxidant capacity. Analyzes of pH, total sugars, acetic acid, ethanol, and microbiological characterization of final formulations were also carried out. For the first fermentation, were found values of phenolic compounds and antioxidant capacity of 30.60 ± 0.93 mg EAG/L and 295.02 ± 5.59 µmol ET/mL, and the formulation with tapereba showed the highest values for total phenolic compounds (34.92 ± 12.25 mg EAG/L), antioxidant capacity (320.57 ± 9.53 µmol ET/mL) and vitamin C (198.25 mg/100g). Thus, the formulations developed had a crucial nutritional appeal to stimulate consumption by the population, in addition to enabling the valorization and addition of commercial value to the Amazonian fruits used.

A Comprehensive Review on the Role of Polymers in Ocular Drug Delivery.

Amongst different routes of drug delivery systems, ophthalmic drug delivery still requires a careful investigation and strict parameter measurements because the eyes are one of the most sensitive parts of the body and require special attention. The conventional systems for eyes lead to rapid elimination of formulation and hence very small contact time on the ocular epithelium. The current review article covers various types of polymers used in ocular drug delivery along with their applications/ limitations. Polymers are widely used by researchers in prodrug techniques and as a penetration enhancer in ocular delivery. This article covers the role and use of different polymeric systems which makes the final formulation a promising candidate for ophthalmic drug delivery. The researchers are still facing multiple challenges in order to maintain the therapeutic concentration of the drug in the eyes because of its complex structure. There are several barriers that further restrict the intraocular entry of the drug. In order to remove/reduce such challenges, these days various types of polymers are used for ocular delivery in order to develop different drug carrier systems for better efficacy and stability. The polymers used are highly helpful in increasing residence time by increasing the viscosity at the ocular epithelium layer. Such preparations also get easily permeated in ocular cells. The combination of different polymeric properties makes the final formulation stable with prolonged retention, high viscosity, high permeability, and better bioavailability, making the final formulation a promising candidate for ocular drug delivery.

Intranasally Delivered Adenoviral Vector Protects Chickens against Newcastle Disease Virus: Vaccine Manufacturing and Stability Assessments for Liquid and Lyophilized Formulations.

Newcastle disease (ND) remains a critical disease affecting poultry in sub-Saharan Africa. In some countries, repeated outbreaks have a major impact on local economies and food security. Recently, we developed an adenovirus-vectored vaccine encoding the Fusion protein from an Ethiopian isolate of Newcastle disease virus (NDV). The adenoviral vector was designed, and a manufacturing process was developed in the context of the Livestock Vaccine Innovation Fund initiative funded by the International Development Research Centre (IDRC) of Canada. The industrially relevant recombinant vaccine technology platform is being transferred to the National Veterinary Institute (Ethiopia) for veterinary applications. Here, a manufacturing process using HEK293SF suspension cells cultured in stirred-tank bioreactors for the vaccine production is proposed. Taking into consideration supply chain limitations, options for serum-free media selection were evaluated. A streamlined downstream process including a filtration, an ultrafiltration, and a concentration step was developed. With high volumetric yields (infectious titers up to 5 × 109 TCID50/mL) in the culture supernatant, the final formulations were prepared at 1010 TCID50/mL, either in liquid or lyophilized forms. The liquid formulation was suitable and safe for mucosal vaccination and was stable for 1 week at 37 °C. Both the liquid and lyophilized formulations were stable after 6 months of storage at 4 °C. We demonstrate that the instillation of the adenoviral vector through the nasal cavity can confer protection to chickens against a lethal challenge with NDV. Overall, a manufacturing process for the adenovirus-vectored vaccine was developed, and protective doses were determined using a convenient route of delivery. Formulation and storage conditions were established, and quality control protocols were implemented.

Safety Assessment of Hops as Used in Cosmetics.

The Expert Panel for Cosmetic Ingredient Safety (Panel) assessed the safety of Humulus Lupulus (Hops) Extract (reported functions include antimicrobial agent and hair conditioning agent) and Humulus Lupulus (Hops) Oil (reported function is fragrance). The Panel reviewed the relevant data related to these ingredients. Because final product formulations may contain multiple botanicals, each containing the same constituents of concern, formulators are advised to be aware of these constituents and to avoid reaching levels that may be hazardous to consumers. For these ingredients, the Panel was concerned about the presence of 8-prenylnaringenin, β-myrcene, and quercetin in cosmetics, which could result in estrogenic effects, dermal irritation, and genotoxicity, respectively. Industry should use current good manufacturing practices to limit impurities and constituents of concern. The Panel concluded that Humulus Lupulus (Hops) Extract and Humulus Lupulus (Hops) Oil are safe in cosmetics in the present practices of use and concentration when formulated to be non-sensitizing.

Splitting for strength: Manipulating polymerization reactor split ratios to control mechanical and rheological properties in bimodal polyethylene resins

AbstractThis study integrates advanced mathematical modeling and experimental methodologies to investigate the simultaneous impact of modifications in the split ratio and molecular weight (MW) of chains on the rheological and mechanical properties of bimodal polyethylene (BiPE) resins. The outcomes underscored the viability of fine‐tuning the molecular weight distribution (MWD) of a BiPE resin by augmenting the MW of high molecular weight (HMW) chains while simultaneously diminishing their proportion in the final alloy formulation. In addition, the experimental results illuminated the prospect of attaining a targeted melt flow index for the final polymers by elevating the MW of HMW chains alongside an increase in the proportion of low molecular weight chains. Significantly, these adjustments resulted in remarkable enhancements in the shear thinning index and strain hardening modulus of the fabricated resins.

Synergistic effect of Tween 20 and TESPT compatibilizers on the performance characteristics of latex imprinted silica-reinforced green tyre tread formulation

The present study has a prime goal to develop a green tyre tread formulation with enhanced performance characteristics including low rolling resistance, improved wet grip, low heat build-up and enhanced mechanical properties which are essential for a high-performance tyre tread compound. A base formulation of natural rubber/polybutadiene (NR/BR) blend with minimum carbon filler was formulated initially without compromising the physical properties much by balancing the properties by incorporating precipitated silica. Enhanced surface area for silica was obtained through the latex imprinting method which had an ultimate effect on the interaction between the matrix macromolecules and filler particles positively. Further, ENR was used as a compatibilizing agent to upgrade physical properties in terms of 20% improvement in tensile and around 10% improvement in tear strength. Additional improvement in physical as well as rolling resistance performance was achieved via the incorporation of coupling agents including TESPT and polyoxyethylene(20) sorbitan monolaurate (Tween 20). Apart from the improvement in mechanical properties, rolling resistance and heat build-up properties are promising for the final tyre tread formulation as both the values tend to reduce considerably by 35% and 63% respectively concerning the base formulation.

A Comparative Investigation of Sibawayh and Jakobson in Functional Linguistics

The objective of this research is to connect Arabic theoretical linguistics with modern linguistics, not by disregarding the present and attributing the later theories solely to Arab grammarians and rhetoricians, as has often been assumed. Rather, this research aims to qualitatively explore the linguistic accomplishments of ancient Arab scholars from a contemporary perspective and identify commonalities and controversies between past and present perspectives. Specifically, this study focuses on Sibawayh's interpretation of functional linguistics and its final formulation by Jakobson. Additionally, the study aims to analyse and compare the principles of language and grammar advocated by ancient Arab linguists and contemporary linguists to deepen our understanding of language and its role in human society. The results of this study reveal that while Sibawayh concentrated on the analysis of structure and function in Arabic grammar, modern linguists such as Jakobson have broadened their approach to include a wider range of perspectives including sociolinguistics, psycholinguistics, and neurolinguistics. Therefore, it is essential to acknowledge the contributions of Sibawayh as his work formed the foundation for language theories in general and linguistics in particular.

Development and In-Vitro Evaluation of Eugenol-Based Nanostructured Lipid Carriers for Effectual Topical Treatment Against C. albicans

The main objective of the experiment is to develop and evaluate hydrogel-bearing nanostructured lipid carriers (NLCs) loaded with ketoconazole (KTZ) for the effective treatment of candidiasis. The eugenol was used as a liquid lipid (excipient) for the development of KTZ-loaded NLCs and was explored for anti-fungal effect. The production of NLCs involves high energy processes to generate spherical, uniform particles, having a higher percentage of entrapment efficiency (%EE) for KTZ with 89.83 ± 2.31 %. The data from differential scanning calorimeter (DSC), powder x-ray diffraction (PXRD), and attenuated total reflectance (ATR) demonstrated the KTZ dispersion in NLCs. The NLCs loaded hydrogel possessed optimum spreadability and exhibited shear thinning behavior, indicating the ease of application of the final formulation. The 6.41-fold higher transdermal flux (Jss) was governed for KTZ from KTZ-NLC than coarse-KTZ, which explains the usefulness of NLCs. The KTZ-NLCs exhibited significant 2.58 and 6.35-fold higher retention in the stratum corneum and viable epidermis of the skin. The cell cytotoxicity studies using human dermal fibroblast cell (HDFS) lines depicted the usefulness of NLCs in reducing cell toxicities for KTZ. The KTZ-NLCs were found to inhibit planktonic growth and hyphal transition and showed a larger zone of inhibition against C. albicans strains with a MIC-50 value of 0.39 μg/mL. The antibiofilm activity of KTZ-NLCs at lower concentrations, in contrast to plain KTZ, explained the interaction of developed NLCs with fungal membranes. The overall results depicted the effectiveness of the loading KTZ in the lipid matrix to achieve antifungal activity against C. albicans.

Optimized, automated and cGMP-compliant synthesis of the HER2 targeting [68Ga]Ga-ABY-025 tracer

BackgroundThe Affibody molecule, ABY-025, has demonstrated utility to detect human epidermal growth factor receptor 2 (HER2) in vivo, either radiolabelled with indium-111 (111In) or gallium-68 (68Ga). Using the latter, 68Ga, is preferred due to its use in positron emission tomography with superior resolution and quantifying capabilities in the clinical setting compared to 111In. For an ongoing phase II study (NCT05619016) evaluating ABY-025 for detecting HER2-low lesions and selection of patients for HER2-targeted treatment, the aim was to optimize an automated and cGMP-compliant radiosynthesis of [68Ga]Ga-ABY-025.[68Ga]Ga-ABY-025 was produced on a synthesis module, Modular-Lab PharmTracer (Eckert & Ziegler), commonly used for 68Ga-labelings. The radiotracer has previously been radiolabeled on this module, but to streamline the production, the method was optimized. Steps requiring manual interactions to the radiolabeling procedure were minimized including a convenient and automated pre-concentration of the 68Ga-eluate and a simplified automated final formulation procedure. Every part of the radiopharmaceutical production was carefully developed to gain robustness and to avoid any operator bound variations to the manufacturing. The optimized production method was successfully applied for 68Ga-labeling of another radiotracer, verifying its versatility as a universal and robust method for radiosynthesis of Affibody-based peptides.ResultsA simplified and optimized automated cGMP-compliant radiosynthesis method of [68Ga]Ga-ABY-025 was developed. With a decay corrected radiochemical yield of 44 ± 2%, a radiochemical purity (RCP) of 98 ± 1%, and with an RCP stability of 98 ± 1% at 2 h after production, the method was found highly reproducible. The production method also showed comparable results when implemented for radiolabeling another similar peptide.ConclusionThe improvements made for the radiosynthesis of [68Ga]Ga-ABY-025, including introducing a pre-concentration of the 68Ga-eluate, aimed to utilize the full potential of the 68Ge/68Ga generator radioactivity output, thereby reducing radioactivity wastage. Furthermore, reducing the number of manually performed preparative steps prior to the radiosynthesis, not only minimized the risk of potential human/operator errors but also enhanced the process’ robustness. The successful application of this optimized radiosynthesis method to another similar peptide underscores its versatility, suggesting that our method can be adopted for 68Ga-labeling radiotracers based on Affibody molecules in general.Trial registration: NCT, NCT05619016, Registered 7 November 2022, https://clinicaltrials.gov/study/NCT05619016?term=HER2&cond=ABY025&rank=1

Curcumin-loaded porous particles functionalized with pH-responsive cell-penetrating peptide for colorectal cancer targeted drug delivery.

The anticancer properties of curcumin have been broadly examined in several shapes, such as nanoparticles and nanocomposite structures. Despite its benefits, curcumin also has some disadvantages, including rapid metabolism, poor absorption, and rapid systemic excretion. Therefore, numerous strategies have been used to increase curcumin's bioavailability. One of these approaches is the use of porous particles like aerogels as drug carriers. Aerogels are special due to their peculiar physical structure. They have a high specific surface area, a significant amount of porosity, and a solid composition, which make them a good choice for drug delivery systems. In the present study, a pH-sensitive aerogel was constructed and evaluated for targeted drug delivery of curcumin to colon cancer. To control the release of curcumin, trehalose was used as a coating agent, and PLP (poly(l-lysine isophthalamide)) was used as a targeted drug delivery agent. PLP is a pseudo-peptidic polymer that increases the cell permeability. In order to investigate and compare the synthesized aerogel before and after loading curcumin and coating with trehalose, physicochemical characterization analyses were performed. Finally, the efficacy of the final formulation was evaluated on HT29 colon cells using the cell bioavailability test. The results indicated the successful synthesis of the aerogel with porous structure with solitary cavities. The trehalose coating performed well, preventing drug release at lower pH but allowing the drug to be released at its intended site. The designed curcumin-loaded porous particles functionalized with PLP showed significant efficacy due to increasing penetration of curcumin into cells, and has potential for use as a new drug carrier with dual effectivity in cancer therapy.

A Stable Formulation of a Non-Steroidal Anti-inflammatory Drug, Ibuprofen and an Antihistamine drug, Famotidine for a Combination Therapy

Purpose: The present research study was focused on developing an oral dosage form with two highly incompatible drugs, a non-steroidal anti-inflammatory drug, Ibuprofen and an antihistamine drug, Famotidine to be administered as a combination therapy in a single dose and further asses the stability of the finished product. Methods: A novel drug formulation was designed by employing mini tablets technology to manufacture Famotidine core tablets and the core tablets are further film coated with Opadry II coating solution to inhibit Famotidine contact with Ibuprofen matrix. Film coated Famotidine 30 mg mini-tablets were then encapsulated in Ibuprofen blend to improve the compatibility and stability of the drug product [1,2]. Each mini-tablet of Famotidine contain 5 mg dose of Famotidine and 6 such mini-tablets were encapsulated in each size “00” hard gelatin capsule containing Ibuprofen blend equivalent to 800 mg claim. The stability of the finished product was evaluated in accelerated stability conditions to ensure the impurities are well within the Pharmacopeia (USP) assigned limits. Results: The dissolution release of Ibuprofen and Famotidine is higher than 85 % in 15 minutes and is compared against the only available product in the combination therapy, DUEXIS® (Ibuprofen and Famotidine Tablets 800 mg and 26.6 mg). The stability of the final formulation is evaluated by placing the samples in 40°C/75 % RH storage condition for six months and the results of the pharmacopeia (USP) listed specified and unspecified impurities are well not more than 0.5 % w/w of the label claim. Famotidine and Ibuprofen are two highly in-compatible drugs for a combination therapy, and has been a challenge in the field to formulate for a combination therapy to improve patient compliance. The two drugs tend to form impurities at significate levels in direct physical contact during any stage of the manufacturing process.

Safety Assessment of Ginkgo biloba-Derived Ingredients as Used in Cosmetics.

The Expert Panel for Cosmetic Ingredient Safety (Panel) assessed the safety of 10 Ginkgo biloba-derived ingredients, which are most frequently reported to function in cosmetics as skin conditioning agents or antioxidants. The Panel reviewed the available data to determine the safety of these ingredients. Because final product formulations may contain multiple botanicals, each containing the same constituents of concern, formulators are advised to be aware of these constituents and to avoid reaching levels that may be hazardous to consumers. The Panel was concerned about the presence of ginkgolic acid in cosmetics. Industry should use good manufacturing practices to limit impurities. The Panel concluded that 5 Ginkgo biloba leaf-derived ingredients are safe in the present practices of use and concentration described in this safety assessment when formulated to be non-sensitizing; data are insufficient to determine the safety of the remaining 5 ingredients under the intended conditions of use in cosmetic formulations.

Preparation and characterization of vaginal suppository of semisynthetic derivatives of ergot alkaloids cabergoline

BackgroundThere is evidence that vaginal cabergoline can help to prevent ovarian hyperstimulation syndrome. Therefore, the vaginal suppository may be a good choice because it can be administered directly into the vagina and has no adverse effects on the stomach. In this regard we developed a cabergoline suppository as an alternative to cabergoline tablets. Design-Expert was used to determine the most suitable concentrations of PEG 6000/400, and Tween 80 to obtain a stable suppository. Specific ratios of PEG6000/400 and Tween 80 were entered as factors, and release, melting time, and hardness were evaluated as responses. In addition, the final formulation was evaluated for weight changes, pH, drug content, degradation time, deformation time, in vitro drug release, DSC analysis, infrared spectroscopy, and stability properties. ResultsThe suppositories were all smooth and white. They all had a weight that averaged less than 5 %. The formulations showed a pH between 6 and 6.5. The active ingredient content ranged between 79.666 ± 8.54 % and 99.67 ± 6.55 %. Suppository stiffness was between 2.74 ± 0.04 and 4.20 ± 0.03. The decomposition time of the suppositories varied between 11.25 ± 0.15 to 20.19 ± 0.08 min. The deformation time was between 26.11 ± 0.06 to 38.59 ± 0.47 min. Cabergoline content was released over 45 min from formulations of F10 (∼46 %), F2 (∼64 %), F6 (∼69 %), F4 (∼79 %), F1 (∼88 %), and F7 (∼93 %). However, other formulations released more than 95 % within 45 min. ConclusionsAll variables except melting time significantly affected our responses. In vitro studies have indicated that the optimized cabergoline formula could be an excellent alternative to cabergoline oral formulations.

Formulation of double nanoemulsions based on pH-sensitive poly acrylic acid/agarose/ZnO for quercetin controlled release

Quercetin (QC) is a promising cancer drug, though its poor solubility and quick release reduce its bioavailability, thus limiting its current applications. In this research, a new hydrogel nanocomposite comprising zinc oxide nanoparticles (ZnONPs), agarose, and polyacrylic acid (PAA), was designed to load QC. Spherical nanocarriers were prepared via environmentally friendly and simple double emulsion approach by injecting PAA/Aga/ZnONPs coated by SPAN 80 surfactant to a hydrophobic olive oil phase. The nanoemulsions were characterized by different techniques to assess the impact of ZnONPs on PAA/Aga pH-sensitive hydrogel as a novel platform for direct administration of QC. FTIR and XRD analysis confirmed the presence of all the nanocomposite components in the final formulation. FE-SEM images revealed the spherical shape and surface homogeneity of the nanocarriers, and zeta potential measurements corroborated their colloidal stability. The addition of ZnONPS increased the drug loading from 41.25% to 47.50% and the encapsulation efficiency from 83.0% to 87.25%. A slower drug release was observed at pH 7.4 for periods of time shorter than 96 h, corroborating the pH-sensitivity of the nanoemulsions. Drug release data at pH 5.4 fitted well to the First-order equation, while at pH 7.4 were better described by the Korsmeyer Peppas model. The reduction in MCF7 living cells in the presence of PAA/Aga/ZnONPs compared to PAA/Aga and the control sample indicates the in vitro cytotoxicity of ZnONPs. The number of late apoptotic cells in PAA/Aga/ZnONPs/QC (37.55%) was higher than that of the other formulations (ZnONPs, PAA/Aga and PAA/Aga/ZnONPs), which may be due to the controlled and slow release of QC from PAA/Aga/ZnONPs/QC. Therefore, these green, biocompatible and biodegradable nanoemulsions show great potential as nanocarriers for QC loading and sustained release against breast cancer.