Ultra Moisturizing Anti-Wrinkle Lotion Enriched with Tocotrienols

A stable palm-based anti-wrinkle lotion enriched with tocotrienols was successfully prepared. The stability of the product was due to the presence of liquid crystalline structure in the emulsion system. It helps in bringing the active to the dermis layer. Functionality active ingredients such as tocotrienols and anti-wrinkle were added in the formulation. A commercial plant extract was used to strengthen the collagen seated at the dermis layer. The product was formulated to pH 5.5 which is suitable for the skin. The mean droplet size is 10.2 µm with a monomodal distribution pattern which prevents agglomeration. This will decrease Brownian motion, thus prolonging its stability. Long-term acute moisturizing tests show a significant increase of between 24% and 17% hydration for five and six weeks respectively. The efficacy testing on 12 subjects confirmed a reduction in natural fine wrinkles on faces during aging or premature aging at ?7.6%.     

Formulation studies on a topical gel of tretinoin�Cdimethyl-beta-cyclodextrin complex

The aim of this work was to develop and characterize a 0.05% tretinoin hydrogel formulations in which tretinoin is free or complexed with dimethyl-beta-cyclodextrin in order to compare the main advantages of its complexation. Theoretically, the complexation will mainly allow to: overcome drug low solubility in water and low stability; enhance the drug release by promoting skin absorption and alleviate of drug inducing local irritation. The hydrogels prepared were both microbiological and physically stable during 30 days. However, the chemical stability was less encouraging. The complexed tretinoin gel had also a higher releasing profile than the free tretinoin gel. This study has demonstrated that it is possible to obtain a microbiological and physically stable gel formulation with good releasing profile.     

Submicron Size Formulation of Linseed Oil Containing Omega-3 Fatty Acid for Topical Delivery

The aim of the present study was to design and develop topical submicron size gel formulation of linseed oil with enhanced permeation through the skin for the management of psoriasis. Linseed oil contains significant amount of α-linolenic acid (ALA) an omega-3 fatty acid, which is responsible for its pharmacological actions. In order to enhance permeation through skin, microemulsion based gel formulation was prepared and characterized. Microemulsions were prepared by aqueous phase titration method, using linseed oil, Unitop 100, PEG 400, and distilled water as the oil phase, surfactant, cosurfactant and aqueous phase, respectively. Selected formulations were subjected to physical stability studies and consequently in vitro skin permeation studies. Surface morphology studies of optimized formulation were done by transmission electron microscopy (TEM). The droplet size of microemulsions ranged from 70 to 500 nm with average particle size 186 nm. The optimized microemulsion was converted into hydrogel using carbopol 971 which had a viscosity of 498 ± 0.04 cps. During in vitro permeation study the flux of microemulsion formulation and gel was found to be 19.05 and 10.2 µg/cm²/hr, respectively, which indicated better penetration of linseed oil through the skin. These result indicated that the developed ME formulation may be a good approach for topical therapy for the management of psoriasis.     

Collagen Hydrolysate Prepared from Chicken By-Product as a Functional Polymer in Cosmetic Formulation

Chicken stomachs can be processed into collagen hydrolysate usable in cosmetic products. The aim of the study was to verify the effects of a carbopol gel formulation enriched with 1.0% (w/w) chicken hydrolysate on the properties of the skin in the periorbital area after regular application twice a day for eight weeks in volunteers ageed 50 ± 9 years. Skin hydration, transepidermal water loss (TEWL), skin elasticity and skin relief were evaluated. Overall, skin hydration increased by 11.82% and 9.45%, TEWL decreased by 25.70% and 17.80% (always reported for the right and left area). Generally, there was an increase in skin elasticity, a decrease in skin roughness, as the resonance times decreased by 85%. The average reduction of wrinkles was 35.40% on the right and 41.20% on the left. For all results, it can be seen that the longer the cosmetic gel formulation is applied, the better the results. Due to the positive effect on the quality and functionality of the skin, it is possible to apply the cosmetic gel formulation in the periorbital area. The advantage of the product with chicken collagen hydrolysate is also the biocompatibility with the skin and the biodegradability of the formulation.     

Evaluation of nanoherbal gel for anti-warts activity

In the present experimental investigation a novel nanoherbal gel containing iron nanoparticles and extract from Cuscuta reflexa was used as a drug. Synthesized nanoherbal increased the drug solubility and penetration in the skin and is useful as a novel delivery system for better anti-warts activity. The experimental work includes preformulation studies of drug (Cuscuta reflexa) which include organoleptic properties, identification and solubility studies. Spectroscopy characterization was performed for identification of drug. The iron nanoparticles were evaluated for their characteristic such as appearance, viscosity and odor. Various formulations F1–F5 was prepared using different formulation variables based on experiment design. The result showed that the formulation F-5 provide the better release using 5.5 pH acetate buffer and at 37 °C temperature for anti-warts activity. The maximum drug release through synthesized nanoherbal gel was found to be 91.3%. Nanoherbal formulation was evaluated for physical appearance, pH, consistency, spreadibility and drug content. Stability study of formulation F5 was carried out for a period of 3 months to determine the percentage release and the results revealed that the formulation is stable under varied humidity and temperature condition and there was no major change in the amount of drug release during the storage condition, which reflected the stability of F5 formulation.     

A Stability Indicating HPLC Assay for Prednisolone Sodium Phosphate in Implantable Infusion Pumps

Abstract

A stability indicting assay for prednisolone sodium phosphate (PSP) in solutions for implantable infusion pumps was developed. PSP and its major breakdown product, prednisolone, were separated from formulation excipients by reverse phase chromatography on a phenyl-bonded phase column using an acetonitrile-phosphate buffer mobile phase. Detection was by ultraviolet absorbance at 243 mm. Recovery from a synthetic formulation was 101.0 ± 0.4% (n=6). The method was used to monitor the stability of PSP solutions in implantable infusion pumps maintained at 37°C over a 21 day period.     

In vitro solar protection factor,antioxidant activity,and stability of a topical formulation containing Benitaka grape (Vitis vinifera L.) peel extract

Abstract

A flavonoid enriched extract (FE) was obtained from grape peels, and in vitro SPF, antioxidant activity, and effects on cell viability of this extract were tested with the intent to develop a cosmetic product. A formulation was developed with the FE, and the stability of this mixture was evaluated in terms of pH, density, viscosity, and SPF (90-days). FE showed no cytotoxicity to human keratinocytes and an in vitro SPF of 18.56 (UV-spectrophotometry). Further, FE showed a UVA protection factor of 3.17?±?0.2, a critical wavelength of 318.0?±?0.1 and a UVA/UVB of 0.9. Antioxidant activity assays resulted in 92.08% and 86.85% of activity against DPPH and ABTS (IC₅₀ = 296.90?±?1.2?µg/mL and 643.13?±?0.9?µg/mL), respectively. Finally, SPF of formulation with FE was 12.45. Results from the in vitro SPF and product stability tests (especially storage under refrigeration), indicate that FE is a promising compound for use as an innovative sunscreen formulation.     

Effect of the moisture content in aerosol on the spray performance of Stmerin ® D hydrofluoroalkane preparations (2)

The spray performance of the new Stmerin? D pressurized metered dose inhalers (MDIs), prescribed for asthma treatment, was previously reported to be sensitive to moisture content in the canister. In this formulation, active ingredients were suspended in hydrofluoroalkanes (HFA-134a and HFA-227). Here, we report on the critical moisture content of a new MDI formulation using HFA-227. We prepared MDIs with different moisture contents (107-331 ppm) and investigated the effect of moisture content on the fine particle dose (FPD). When the moisture content exceeded 280 ppm, FPD was reduced by 20%. The moisture content can be kept below this level by controlling moisture ingress with selected sealing gasket materials and by controlling the manufacturing conditions. The long-term stability and moisture penetration rate at 25°C and 60% relative humidity (RH) of the new HFA-227 formulation were tested over 36 months. Moisture content increased to approximately 210 ppm after 24 months and 230 ppm after 36 months storage; the drug content did not change over 24 months; FPD was slightly reduced by 24 months but still complied with the product specification. These results demonstrate that the critical moisture content of the Stmerin? D HFA-227 MDI formulation to meet required spray performance is between 280 and 330 ppm, and this formulation (at <210 ppm moisture level) is stable over 24 months.     

Effect of tretinoin inclusion in dimethyl-beta-cyclodextrins on release rate from a hydrogel formulation

The aim of this work was to study the release, permeation and skin retention profiles of 0.05% tretinoin hydrogel formulations in which tretinoin was in free form or complexed with dimethyl-beta-cyclodextrin in a stoichiometry of 1:4. Theoretically, this complexation will mainly allow to: overcome drug’s low water solubility and low stability; enhance the drug permeation by promoting skin absorption and alleviate drug inducing local irritation. In vitro release, permeation and skin retention tests were performed in both formulations in order to compare the main advantages of this complexation. The influence of the thermodynamic activity on the drug release profile was also investigated. This study proved that tretinoin inclusion complexes formulation with excess of cyclodextrins had better release profile than the free tretinoin formulation. It was concluded that in this study, thermodynamic activity was not the driving force for the release rate improvement observed with cyclodextrins. Probably, this improvement was due to the increased availability of tretinoin near the membrane surface. In fact, the percentage of total drug that had been retained in the skin was 0.41?±?0.08% for complexed tretinoin gel and 0.17?±?0.04% for the free tretinoin gel.     

Natural rheological modifiers for personal care

The development of personal care formulations incorporates the deliberation of the prerequisite product rheology and the right rheology modifier to deliver these effects. While the effectiveness of the finished product will hinge on the selection and level of active ingredients and excipients, the esthetics and even the penetration of these actives into the stratum corneum will be affected by the product rheology. Rheology modifiers are frequently denoted as thickeners, and while increasing the apparent viscosity should enhance the perception of quality in a formulation, this is only one aspect of rheological control. The product itself can be Newtonian or pseudoplastic, thixotropic, existing as a ringing gel or a stringy flowable liquid. This changes the way that the product appears in the bottle, the ease with which aliquots are poured or scooped from the packaging, the process of rubbing it into the skin or along the hair shaft, and upon using, the rinsing and removal of the product. It will also be vital to select the correct rheological characteristics to guarantee the stability of the finished formulation. By changing the structure of polymeric rheology modifiers, the impact on the sensorial properties and performance characteristics can be investigated. Careful selection of monomers, structure and other co‐ingredients will result in products optimized for use in skin care formulations. Copyright © 2016 John Wiley & Sons, Ltd.     

Physical Stability and the Droplet Distribution of Rice Oil–in–Water Emulsion

The objective of the current study was to evaluate long-term stability of emulsions with rice oil by assessing their physical properties. For this purpose, six emulsions were prepared, their stability was examined empirically, and the most correctly formulated emulsion composition was determined using a computer simulation. Variable parameters (oil and thickener content) were indicated with optimization software based on Kleeman's method. Synthesized emulsions were studied by numerous techniques involving determination of particle size and distribution of emulsion, optical microscopy, viscosity, and novelty analysis—Turbiscan test.

The emulsion containing 50 g of oil and 1.2 g of thickener had the highest stability. Empirically determined parameters proved to be consistent with the results obtained using the computer software. The computer simulation showed that the most stable emulsion should contain from 35.93 to 50 g of oil and 0.94 to 1.19 g of thickener. The computer software based on Kleeman's method proved to be useful for fast optimization of the composition and providing parameters of stable emulsion systems. Forming emulsions based on rice oil is a chance to introduce a new, interesting representative of functional food as well as a cosmetic product.     

Physicochemical Properties and Storage Stability of Microencapsulated DHA-Rich Oil with Different Wall Materials

This study aimed to evaluate the physicochemical properties and storage stability of microencapsulated DHA-rich oil spray dried with different wall materials: model 1 (modified starch, gum arabic, and maltodextrin), model 2 (soy protein isolate, gum arabic, and maltodextrin), and model 3 (casein, glucose, and lactose). The results indicated that model 3 exhibited the highest microencapsulation efficiency (98.66 %) and emulsion stability (>99 %), with a moisture content and mean particle size of 1.663 % and 14.173 μm, respectively. Differential scanning calorimetry analysis indicated that the Tm of DHA-rich oil microcapsules was high, suggesting that the entire structure of the microcapsules remained stable during thermal processing. A thermogravimetric analysis curve showed that the product lost 5 % of its weight at 172 °C and the wall material started to degrade at 236 °C. The peroxide value of microencapsulated DHA-rich oil remained at one ninth after accelerated oxidation at 45 °C for 8 weeks to that of the unencapsulated DHA-rich oil, thus revealing the promising oxidation stability of DHA-rich oil in microcapsules.     

Benefits of combinations of vitamin A, C and E derivatives in the stability of cosmetic formulations

Chemically stable ester derivatives of vitamins A, C and E have become a focus of interest for their role in the satisfactory results in skin aging treatments. Accordingly, the aim of this study was to evaluate the physical and chemical stability of a cosmetic formulation containing 1% retinyl palmitate, ascorbyl tetraisopalmitate and tocopheryl acetate, alone or in combination. In the studies of physical stability, a Brookfield rheometer was used to determine rheological behavior of formulations containing the vitamins. Chemical stability was determined by HPLC on a Shimadzu system with UV detection. Results showed that formulations had pseudoplastic behavior and that vitamins did not alter their apparent viscosity and thixotropy. In the chemical stability studies, first-order reaction equations were used for determinations of the shelf-life of vitamins derivatives considering a remaining concentration of 85%. Combined vitamins in a single formulation had a slightly lower degradation rate as compared to different preparations containing only one of the vitamins. Considering that many cosmetic formulations contain vitamin combinations it is suggested that the present study may contribute to the development of more stable formulations containing liposoluble vitamins.     

Characterization and evaluation of free and nanostructured ursolic acid incorporated in cosmetic formulation using thermal analysis

The ursolic acid (UA) increases the skin’s barrier function and acts in epidermal differentiation of keratinocytes in the epidermis, promoting cell renewal. Besides the mentioned properties UA also has antioxidant, antimicrobial, and anti-irritant functions to cosmetic formulations. Thus, it is necessary formulation studies to insure the development of quality cosmetic products containing this active, increasing its antioxidant potential within nanoparticles. This study aims to characterize and evaluate the thermal behavior of UA in free and nanostructured forms, and both incorporated into a cosmetic base formulation, using thermogravimetry and differential scanning calorimetry. Through the study were observed that free UA, in the embedded nanoparticles and in base formulation exhibited different behavior in similar thermal profile and relative to the presence of UA. The UA remained stable to a temperature of 250 °C and the technique has been shown to be effective for characterizing UA, evaluate water content, and stability of the formulation base.     

LC Stability Studies of Voriconazole and Structural Elucidation of Its Major Degradation Product

Voriconazole is a broad spectrum agent used to treat serious fungal infections. Stability studies conducted so far refer to the stability of the injectable formulation in different solvents, packaging materials and on storage but studies on the inherent chemical stability of the drug are not available. The purpose of this study was to evaluate the stability of the drug under stress conditions, in solution and in the solid state; isolate and elucidate the structure of the major degradation product and evaluate the antifungal activity of the degradation products. The quantification of the drug after exposure to degradation conditions was studied by a validated LC method. Among the conditions tested, it was found that the drug is more rapidly degraded in an alkaline medium, exposure to UVC radiation (254 nm) and elevated temperatures (60 °C). Degradation was greater under the first two conditions and in solution. Tablets exposed to UVC radiation for 14 days remained chemically and physically stable. For the isolation of the major degradation product, semi-preparative LC was employed and for the structural elucidation, spectroscopic techniques (¹H and ¹³C NMR spectroscopy, IR spectroscopy and mass spectrometry) were used, and the major degradation product identified as 1-(2,4-difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)-1-ethanone. The degraded samples were evaluated through microbiological assay and found to have no antifungal activity.     

Nasal in situ gel containing hydroxy propyl ��-cyclodextrin inclusion complex of artemether: development and in vitro evaluation

The objective of the present investigation was to explore the formulation and evaluation of in situ gel for the nasal delivery of artemether (ARM), a poorly water-soluble antimalarial agent using temperature induced gelation technique using Pluronic with mucoadhesive polymer Hydroxy Propyl Methyl Cellulose (HPMC) K4M in different ratios. Initially, due to low water solubility, an inclusion complex of the antimalarial artemether (ARM) in hydroxypropyl-??-cyclodextrin (HP??CD) was prepared and characterized. The in situ gels so prepared were characterized for its gelation properties, viscosity, gel strength, mucoadhesion, drug content, drug release rate and for its histopathological studies. Pluronic and HPMC based in situ gel (PLH2) showed the effective gelation, viscosity, gel strength and drug release properties along with good mucoadhesive strength, it is further subjected for stability studies carried out at 30 ± 2 °C and 60 ± 5% RH for 90 days in order to know the influence of temperature and relative humidity on drug content and on drug release profile. Histological examination of formulations did not show any remarkable damage to nasal mucosa. The formulation also retained the good stability at accelerated conditions over the period of 90 days. Owing to these properties it can be used as an effective delivery system for the nasal route. These in situ gelling systems would be definitely useful for cerebral malaria.     

Stability and Formulation of Erlotinib in Skin Creams

Recent studies have highlighted the benefit of repurposing oral erlotinib (ERL) treatment in some rare skin diseases such as Olmsted syndrome. The use of a topical ERL skin treatment instead of the currently available ERL tablets may be appealing to treat skin disorders while reducing adverse systemic effects and exposure. A method to prepare 0.2% ERL cream, without resorting to a pure active pharmaceutical ingredient, was developed and the formulation was optimized to improve ERL stability over time. Erlotinib extraction from tablets was incomplete with Transcutol, whereas dimethyl sulfoxide (DMSO) allowed 100% erlotinib recovery. During preliminary studies, ERL was shown to be sensitive to oxidation and acidic pH in solution and when added to selected creams (i.e., Excipial, Nourivan Antiox, Pentravan, and Versatile). The results also showed that use of DMSO (5% v/w), neutral pH, as well as a topical agent containing antioxidant substances (Nourivan Antiox) were key factors to maintain the initial erlotinib concentration. The proposed ERL cream formulation at neutral pH contains a homogeneous amount of ERL and is stable for at least 42 days at room temperature in Nourivan cream with antioxidant properties.     

Study of Stability of Sesame Oil-In-Water Emulsions Determined using an Optical Analyzer and Measurement of Particle Size and Distribution

The aim of the study was to determine the optimal conditions, that is, the content of sesame oil and the amount of carboxymethylcellulose, to obtain stable dispersion systems. Emulsions were stored under different temperature conditions. For this purpose, six emulsions were prepared and their stability was examined empirically using techniques including particle size analysis, optical microscopy, and the Turbiscan test. The emulsion containing 40 g of oil and 0.6 g of thickener had the highest stability. No destabilizations in whole the range of stored temperature were observed for the emulsion with that composition. Emulsion was stable as well at cool temperature as at extreme environment (40°C). Nowadays, the use of O/W emulsions based on vegetable oil is continuously increasing. To date, sesame oil has been used mainly for direct consumption. The present work indicates a novel possibility for use of sesame oil as the fat base of an emulsion system. Besides, the study gave information about parameters of long-term stability emulsion what is the key in the quality of the dispersion systems. This knowledge is necessary for the industry in order to avoid destabilizing processes occurring in a new product.     

Starch cellulose acetate co-acrylate (SCAA) polymer as a drug carrier

The present study aims to create a controlled-release system through the preparation and characterization of starch cellulose acetate co-acrylate (SCAA) polymer for application as a carrier for cancer drugs. SCA was prepared from maize starch and different ratios of cellulose acetate. The obtained product SCA was reacted with acrylic acid monomer to give cellulose acetate co-acrylate. The best ratio of starch to cellulose acetate was found to be 90:10, giving a stable product with acrylic acid. The cancer drug 8-(2-methoxyphenyl)-3,4-dioxo-6-thioxo-3,4,6,7-tetrahydro-2h-pyrimido[6,1-c]-[1,2,4]triazine-9-carbonitrile was dissolved in dimethylformamide then added gradually at the end of the previous reaction under stirring for 15 min. The prepared polymers with and without the drug were characterized by Fourier-transform infrared spectroscopy. Cuboids discs of the prepared polymer/drug were subjected to drug release in aqueous media at different pH values. The release was measured spectrophotometrically. It was found that the release rate depends on the pH of the aqueous medium as well as on the concentration of the drug loaded onto the polymer carrier. Above pH 12, the polymer containing the drug degraded completely within 1 h after being subjected to alkaline media. Sustained release of drug extended to about 20 days. The amount released depended on the pH of the media in the following order: basic media > acidic media > neutral. According to Higuch’s equation, the diffusion coefficient was found to be 4.2 × 10^?8 and 5.5 × 10^?8 cm s^?1 for the two evaluated concentrations (1.5 and 2 %) of active organic compound (drug).     

Stability studies on nifedipine tablets using thermogravimetry and differential scanning calorimetry

A new formulation of nifedipine tablets was prepared. The tablets were conditioned in amber-colored glass containers and placed in a climatized room at 40 °C and relative humidity of 75% for 180 days. Differential scanning calorimetry (DSC) and Thermogravimetry (TG) were used in order to evaluate the thermal properties of nifedipine, the excipients and two well-known nifedipine degradation products. There is no evidence of interaction between nifedipine and excipients or degradation products. High performance liquid chromatography (HPLC) was used in the dosage of nifedipine tablets before and after acclimatized exposure. Results show that DSC and TG offer important data for a more detailed assessment of the stability of a pharmaceutical formulation.