Cetyl Research Articles

Effect of Lipid Additives and Drug on the Rheological Properties of Molten Paraffin Wax, Degree of Surface Drug Coating, and Drug Release in Spray-Congealed Microparticles.

Paraffin wax is potentially useful for producing spray-congealed drug-loaded microparticles with sustained-release and taste-masking properties. To date, there is little information about the effects of blending lipids with paraffin wax on the melt viscosity. In addition, drug particles may not be entirely coated by the paraffin wax matrix. In this study, drug-loaded paraffin wax microparticles were produced by spray-congealing, and the effects of lipid additives on the microparticle production were investigated. The influence of lipid additives (stearic acid, cetyl alcohol, or cetyl esters) and drug (paracetamol) on the rheological properties of paraffin wax were elucidated. Fourier transform-infrared spectroscopy was conducted to investigate the interactions between the blend constituents. Selected formulations were spray-congealed, and the microparticles produced were characterized for their size, drug content, degree of surface drug coating, and drug release. The viscosity of wax-lipid blends was found to be mostly lower than the weighted viscosity when interactions occurred between the blend constituents. Molten paraffin wax exhibited Newtonian flow, which was transformed to plastic flow by paracetamol and pseudoplastic flow by the lipid additive. The viscosity was decreased with lipid added. Compared to plain wax, wax-lipid blends produced smaller spray-congealed microparticles. Drug content remained high. Degree of surface drug coating and drug release were also higher. The lipid additives altered the rheological properties and hydrophobicity of the melt and are useful for modifying the microparticle properties.

Alkenones as a Promising Green Alternative for Waxes in Cosmetics and Personal Care Products

The move toward green, sustainable, natural products has been growing in the cosmetic and personal care industry. Ingredients derived from marine organisms and algae are present in many cosmetic products. In this study, a new green ingredient, a wax (i.e., long-chain alkenones) derived from Isochyrsis sp., was evaluated as an alternative for cosmetic waxes. First, the melting point was determined (71.1–77.4 °C), then the alkenones’ thickening capability in five emollients was evaluated and compared to microcrystalline wax and ozokerite. Alkenones were compatible with three emollients and thickened the emollients similarly to the other waxes. Then, lipsticks and lip balms were formulated with and without alkenones. All products remained stable at room temperature for 10 weeks. Lipstick formulated with alkenones was the most resistant to high temperature. Finally, alkenones were compared to three cosmetic thickening waxes in creams. Viscosity, rheology, and stability of the creams were evaluated. All creams had a gel-like behavior. Both viscosity and storage modulus increased in the same order: cream with alkenones < cetyl alcohol < stearic acid < glyceryl monostearate. Overall, alkenones’ performance was comparable to the other three waxes. Alkenones can thus offer a potential green choice as a new cosmetic structuring agent.

Formulation and physical stability test of oleanolic acid cream and gel

Plantago major has been empirically used for wound healing. One of its chemical compounds, oleanolic acid, exhibited wound healing activity on hyperglycemic rats. The aims of this study were to (1) formulate oleanolic acid into topical dosage forms i.e. cream and gel; and (2) evaluate the physical stability of the products. Oleanolic acid was formulated into the dosage forms using stearic acid, isopropyl palmitate and cetyl alcohol as the cream base and carbomer as the gel base. Cream and gel were then subjected into accelerated (40±2°C/75±5% RH) and room temperature (27±2°C/73±5% RH) stability test for six weeks. Physical stability was determined using parameters of visual appearance, specific gravity, viscosity and flow properties, for both gel and cream, as well as the type of emulsion and particle size for the cream. Data analysis were performed using one-way ANOVA and paired t-test. It is concluded that gel and cream of oleanolic acid were able to maintain their visual appearance, specific gravity, viscosity and flow properties during six weeks of storage. In addition, oleanolic acid cream could also maintain its particle size and type of emulsion during testing.

Effect of CaCl2 on the Evaporation Reduction ability of Cetyl Alcohol

Effect of CaCl2 on the Evaporation Reduction ability of Cetyl Alcohol

Enzymatic kinetics of cetyl palmitate synthesis in a solvent-free system

Cetyl palmitate was synthetized by esterification the cetyl alcohol with palmitic acid in a solvent-free system. Reactions were performed in batch mode using commercial lipase Lipozyme RM IM as catalyst. Stirring speed (180, 480 and 720 rpm), temperature (60, 70, 80 and 87 °C), amount of catalyst (0.5, 1.0 and 1.5% wt% related to the mass of substrates) and alcohol:acid molar ratio (0.5:1, 1:1 and 2:1) were evaluated and best reaction conditions obtained were 480 rpm, 70 °C, 1.0% of enzyme and 1:1 M ratio. A novel kinetic model based on random-sequential bi-bi mechanism was proposed and showed a good agreement with experimental data. Furthermore, this model was proved to be suitable for kinetics predictions with a small uncertainty. The catalyst was recycled and showed good stability since reaction conversion decreased only 6.8% after 15 reuses.

Antimicrobial peptide-loaded liquid crystalline precursor bioadhesive system for the prevention of dental caries.

BackgroundAnticaries agents must interfere with the adhesion of Streptococcus mutans and its proliferation in dental biofilm, without causing host toxicity and bacterial resistance. Natural substances, including cationic antimicrobial peptides (CAMPs) and their fragments, such as β-defensin-3 peptide fragment (D1–23), have been widely studied. However, the chemical and physical stability of CAMPs may be compromised by external factors, such as temperature and pH, reducing the period of antimicrobial activity.MethodsTo overcome the aforementioned disadvantage, this study developed and character-ized a drug delivery system and evaluated the cytotoxicity and effect against S. mutans biofilm of a D1–23-loaded bioadhesive liquid crystalline system (LCS). LCS was composed of oleic acid, polyoxypropylene-(5)-polyoxyethylene-(20)-cetyl alcohol, Carbopol® 974P and Carbopol® 971P. LCS was analyzed by polarized light microscopy (PLM), rheology (viscoelasticity and flow properties) and in vitro bioadhesion. The viability of epithelial cells was evaluated. Minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) against S. mutans were determined for D1–23 for further evaluation of the effect against S. mutans biofilm after 4 and 24 h of exposure to treatments.ResultsPLM, rheology, and in vitro bioadhesion tests showed that both viscosity and bioadhesion of LCS increased after it was diluted with artificial saliva. D1–23-loaded LCS system presented better activity against S. mutans biofilm after 24 h when compared to 4 h of treatment, showing a cumulative effect. Neither LCS nor D1–23-loaded LCS presented toxicity on human epithelial cells.ConclusionD1–23-loaded LCS is a promising drug delivery system for the prevention of dental caries.

The usage of Jati Leaves Extract (Tectona grandis L.f) As color of lipstick

Lipstick is one of the most used cosmetics by women. According to Tranggano and Latifah (2007), lipstick is a cosmetic applied to the lips, to protect the lips in cold and dry air so that the lips are not easy to dry and crack. Lipstick is used by women for a long time so that lipstick should be safe and do not cause irritation. Chemicals substances in the manufacture of lipstick can accidentally be consumed and long-term use so that its accumulation in the body would be harmful to health. Synthetic lipstick color is one part of the dangerous lipstick making material. Synthetic substances can be replaced with natural dyes. The use of natural dye limits on cosmetics is 5-15% (Mercado, 1991). One example of natural dyes that can be used is the dye from the Jati leaves (Tectona grandis L.f). This study aim is to prove that Jati leaves (Tectona grandis L.f) can be used as a natural dye in the material of lipstick. The method used in this research is the method of extraction maceration with jati leaf samples of 300 grams and ethanol of 96%. Component of lipstick formula which are cera alba, lanolin, vaseline, cetyl alcohol, paraffin solid, oleum ricini, oleum rosae, propylene glycol, butyl hydroxytoluene, methyl paraben, and the addition Jati leaf extract under the concentration of 0%, 18% , and 22%. The material of lipstick is easy to apply, stable, brown color, homogeneous, melting point of 600C, range pH between 3 at 4 and lipstick have a breaking point of 500 grams. Jati leaf extract (Tectona grandis L.f) can be used as a dye or color of lipstick.

Hot melt granulation method for the preparation of floating matrix tablets of Tolperison Hydrochloride

Tolperisone HCl is a centrally muscles relaxant drug. It is a highly water-soluble drug. It has a biological half-life of 1.5–2.5 h. It has absorption window in the small intestine and unstable in intestinal pH 4 to 7. Gastroretentive drug delivery systems have shown to be of better significance in controlling release rate for drug having site specific absorption. The aim of the present investigation was to develop effervescent floating matrix tablets of Tolperisone Hydrochloride. Cetyl alcohol was selected to prepare hot melt granules (HMG) of Tolperisone HCl. Effervescent floating matrix tablet was prepared using cetyl alcohol as lipophilic surfactant and HPMC K100M as hydrophilic polymers. The HMG based floating matrix tablets were optimized by 32 full factorial design to study the effect of independent variables, i.e. amount of cetyl alcohol (X1) and amount of HPMC K100M (X2) on dependent variables like % swelling index (Y1), time required to 50% drug released(t50)(Y2) and time required for 90% drug release (t90)(Y3). From the regression analysis, it was observed that selected two independent variables show significant effect on response variables. From the results obtained, F10 formulation (58.10 mg of cetyl alcohol, 147.18 mg of HPMC K100M) was selected as optimized batch which showed optimum floating lag time (14 s), drug content (102.78 ± 2.15%), %swelling index (182.63 ± 2.15 at 12 h), t50 (310.2 min) and t90(649.8 min). Thus, the effervescent floating matrix tablets based on HMG is suitable to get site specific delivery and controlled release of Tolperisone HCl.

Positive allelospoly of Melia dubia Cav. spatial geometry improve quantitative and qualitative attributes of Aloe vera L.

Absract Study was conducted to ascertain the positive or negative allelospoly among Melia dubia-Aloe vera as components in silvi-medicinal land use [L1-M. dubia (2 × 2 m) + A. vera; L2-M. dubia (3 × 2 m) + A. vera; L3-M. dubia (4 × 2 m) + A. vera) and L4-sole A. vera] cropping systems. M. dubia spatial geometries resulted significant (P≤ 0.05) effect on quantitative and qualitative attributes of A. vera. Quantitative attributes viz., growth (plant height, mature leaf length, and small, mature and total leaves per plant) and biomass (above and below ground and total biomass, mature leaf, pulp, leaf peel and aloe latex) were significantly higher under M. dubia (2 × 2 m)-A. vera silvi-medicinal land use system (closer spacing) as compared to wider spatial M. dubia geometries and A. vera sole cropping. Growth and biomass decreased with increase in M. dubia spacing with minimum under sole crop of A. vera. No significant effect of silvi-medicinal and sole cropping systems was observed on A. vera below ground biomass. In A. vera pulp, through. Gas Chromatography-Mass Spectrometry, 11, 13, 9 and 9 different phytochemicals were detected in M. dubia (2 × 2 m) + A. vera; M. dubia (3 × 2 m) + A. vera and M. dubia (4 × 2 m) + A. vera) and A. vera sole cropping systems, respectively. Percentage of some of the phytochemicals [+(-salsolidine); cetyl alcohol, myristic acid, cyclopentane and 5-triazole, 3ethyl was less under closest spacing (2 × 2 m) and sole cropping system; however in wider spacing (3 × 2 and 4 × 2 m) percentage of these phytochemicals was higher. Intercropping of A. vera significantly affected the growth of M. dubia; however, there was no such effect on volume and biomass production when extrapolated to hectare basis. This study substantiate that M. dubia spatial geometries had positive allelospoly on A. vera growth, biomass and phytochemicals in A. vera pulp. Hence, tree spatial geometry is essential parameters to be considered for growing medicinal plants under agroforestry systems.

Design and optimization of gastro-floating sustained-release tablet of pregabalin: In vitro and in vivo evaluation

Pregabalin is a promising drug for the treatment of neuropathic pain, a chronic disease affecting a large population needing long-term treatment. However, due to its short half-life, the commercial tablet has to be administered 2–3 times per day, with inconvenience for patient and fluctuations of plasma concentration. In this study, a gastro-floating drug delivery system of pregabalin was developed to prolong the gastric retention of drugs absorbed or act in stomach or upper gastrointestinal tract. First of all, it was proved that the drug was mainly absorbed in stomach and upper gastrointestinal tract. The final formulation was optimized in consideration of buoyancy and drug release profile. The gastro-floating tablet was prepared with hydroxypropyl methylcellulose (HPMC) as sustained-release matrix, lipophilic cetyl alcohol as floating-assistance agent and other excipients to achieve satisfying buoyancy and sustained release performance with mechanisms of diffusion and matrix erosion. Food exhibited significant effect on the pharmacokinetics of gastro-floating tablet and conventional capsule. Compared with conventional capsules, the relative bioavailability of gastro-floating tablet in fasted conditions or in fed conditions was only 62.47 ± 10.80% and 100.98 ± 17.25% respectively, even though the gastro-floating tablet obtained decreased Cmax and prolonged Tmax in fasted and fed conditions. Besides, good in vivo-in vitro correlation of the gastro-floating tablet was established. In summary, a gastro-floating tablet of pregabalin exhibiting desired buoyancy and release profiles was designed, and the tablet expressed significantly sustained-release behavior in fed conditions with good in vivo-in vitro correlation. The designed gastro-floating system is a promising choice for the patients to relieve neuropathic pain.

A novel optimized mold release oil-in-water emulsion for polyurethane foams production

Release agents are compounds usually sprayed on the molds surface, forming a thin film that can act as a barrier preventing the sticking. Herein, both physical and chemical optimization of a wax-based O/W emulsion for polyurethane (PU) foams is reported. E_N1.8Cet1.2Ac2.5 sample (where N, Cet and Ac stand for the percentages of linear amine, cetyl alcohol and acetic acid), emulsified by the inversion point method, turned out to have the optimal composition, in terms of smaller oil droplets size (by Dynamic Light Scattering analysis and optical measurements), long-term stability (by Abbe refractometer and backscattering tests), good spreading (contact angle and surface tension measurements) and low corrosion phenomena (by potentiodynamic polarization tests, Scanning Electron Microscopy analysis). Principal Component Analysis helped to find the best correlations among all the investigated variables and to have some predictions on the role of the different raw materials in affecting the final stability of the emulsions.

Kinetic and thermodynamic studies on the enzymatic synthesis of wax ester catalyzed by lipase immobilized on glutaraldehyde-activated rice husk particles.

Commercial lipase from Thermomyces lanuginosus has been immobilized on glutaraldehyde-activated rice husk particles via covalent attachment. It was reached maximum immobilized protein concentration of 27.5 ± 1.8mgg-1 of dry support using the initial protein loading of 40mgg-1 of support. The immobilized biocatalyst was used to synthesize cetyl oleate (wax ester) via direct esterification of oleic acid and cetyl alcohol. The influence of relevant factors on ester synthesis, such as reaction temperature, biocatalyst concentration, presence or lack of hydrophobic organic solvents, acid:alcohol molar ratio, and reaction time has been evaluated. The experimental data were well fitted to a second-order reversible kinetic model to determine apparent kinetic constants. Thermodynamic studies have revealed that the reaction was a spontaneous and endothermic process. Under optimal experimental conditions, it was observed maximum ester conversion of 90.2 ± 0.6% in 9h of reaction time in hexane medium using 1M of each reactant (cetyl alcohol and oleic acid), at 50°C and biocatalyst concentration of 15% m/v of reaction mixture. Similar conversion (91.5 ± 0.8%) in a solvent-free system was also obtained within 24h of reaction. The biocatalyst retained 85% of its initial activity after 12 cycles within 9h of reaction in hexane medium. The physicochemical properties of purified ester have been determined in accordance with ASTM standards. The results indicate that the prepared biocatalyst has great potential for wax ester synthesis due to its satisfactory catalytic activity and operational stability.

FORMULASI SEDIAAN LIPSTIK EKSTRAK BUNGA ROSELLA (Hibiscus sabdariffa) SEBAGAI PEWARNA DAN MINYAK ZAITUN (Olive oil) SEBAGAI EMOLIEN

Islam is a beautiful religion and loves beauty. The using of a lipstick is to form a lip in an attractive appearance and to protect the lips from dryness with no side effects. The use of rosella as a dye and olive oil as an emollient in the formulation of the preparations due to the red pigments of anthocyanin in rosella (Hisbiscus sabdariffa l.) and olive oil can be used as an emollient to keep the moisture of the lips. The purpose of this study was to make a lipstick with a good stability. The simplisia of rosella flowers was macerated in ethanol 96%. The components of the lipstick used are cera alba petroleum jelly, aba, Cetyl alcohol, lanolin, titanium dioxide, nipagin, oleum rosae, olive oil and extracts of flowers rosella with concentrations of 0%, 2%, 4%, 6%, 8%, 10%. The lipstick mixture was then tested including: homogeneity, stability, grease, melting point and pH tests. Test a fondness and irritation test performed on the 25 panelists. The results showed that the concentrations of rosella extract 0% did not cause any color or white, the concentration of 2%-4% color posed red fade, the concentration of 6% was red, the concentration of 8%-10% was dark red. Concentration of the extract of 0%-4% did not experience the color change (stable) in a storage room temperature for 30 days. As for the material of 6%-10% color lipstick changes slowly, due to the occurrence of oxidation on lipstick. The result of fondness and irritation tests are that in the preparation of 1, 2, 3, 4, 5 and 6 does not cause irritation, itching and skin redness on the skin.

Fatty alcohol containing nanostructured lipid carrier (NLC) for progesterone oral delivery: In vitro and ex vivo studies

This study aims to overcome most of the obstacles that face oral administration of progesterone. Fatty alcohols (cetyl, cetostearyl and 1:1 mixture) containing NLCs were thought to be one of the most relevant systems based on progesterone drawbacks as acid sensitivity and poor solubility. Formulations were prepared characterized for physicochemical evaluation, in vitro release, in vitro stability in gastric fluid, short term stability, interaction possibility and ex vivo permeation studies. The results showed nanorange particle size with major influence of fatty alcohol concentration. In vitro stability in gastric fluid and release results suggested protection of formulation from gastric environment with controlling the drug release as a function of fatty alcohol concentration. Infrared and thermal analyses showed interaction among fatty alcohol, stearic acid and progesterone. Ex vivo results showed that formulations significantly (p < 0.05) permeated through duodenum when compared with suspension after 8 h. The results collectively indicated that the cetyl alcohol containing NLC was a potential drug delivery system for oral administration of progesterone.

Papain Loaded Solid Lipid Nanoparticles for Colorectal Cancer Therapy

Background: Colorectal cancer (CRC) also known as bowl cancer is still one of the leading causes of cancer related mortality worldwide. Generally tumor cells are protecting themselves by fibrin coat and it is resistant to fibrinolytic degradation. Such a coated tumor appears as ‘self' to the immune system, and thus is not detected as a tumor by the immune system (i.e. natural killer cells). Hence, a potent proteolytic enzyme has to propose/ identify to dissolve the protective fibrin layer, exposing the tumor cell surface to chemotherapy and immune attack. In this research papain was considered to be the potential proteolytic agent, can break down the fibrin coat of cancer cell wall and ultimately the cancer cells are exposed to immune attack and help against the cancer. Secondly, the cytotoxic compound(s) directly deliver to cancer site without harm to normal cells. Methods: The attempt made to attain this objective, we were designed to fabricate the Papain loaded solid lipid nanoparticles (SLN) by melt dispersion-ultrasonication technique, and investigate the various formulation parameters. The papain loaded SLN was characterized by particle size analysis, zeta potential analysis, differential scanning calorimetry (DSC), Scanning electron microscopy (SEM), drug encapsulation efficiency, in vitro drug release, and in vitro cytotoxicity studies on HT-29 colorectal cancer cells. Results: The successful outcome of this research was that, the cetyl alcohol based SLN of papain were successfully prepared by using melt dispersion- ultrasonication method with maximum encapsulation efficiency with desired particle size. The release profile of the produced SLN was investigated in phosphate buffer media, and it showed prolonged release during 24 h. The drug release behaviour from the SLNs exhibited a biphasic pattern with the burst release at the initial stage and sustained release subsequently. Future perspective of this research is that need to investigate the SLN for the lymphatic uptake to produce local action on metastatic colorectal cancer. In vitro cell viability for P-SLNs was tested on colorectal Adenocarcinoma HT-29 cells by MTT assay. The results revealed that the in vitro cell viability against different concentrations of papain was 99% and 31 % which were treated with 5µg/ml and 80µg/ml concentration respectively. The cell viability of HT-29 cells was decreased signicantly from 94 % to 17 % treated with P-SLN at 5 µg/ml and 80 µg/ml concentration respectively. Therefore, the papain loaded SLNs exhibits a better performance on getting lower cell viability (or) equivalent high cytotoxicity than that of pure papain. Therefore, the SLNs delivery system plays a significant role in enhancing the cytotoxic efficacy of papain enzyme against colorectal cancer cells. Conclusion: In this research, we successfully formulated the P-SLN for the treatment of colorectal cancer therapy. We investigate the various formulation parameters, drug release profile and cytotoxic efficacy of P-SLN. Upon successful completion of this work, P-SLNs delivery system is predictable to produce enhanced cytotoxic efficacy against HT-29 colorectal cancer cells. The papain loaded SLNs can potentially be utilized as a drug delivery system for the treatment of colorectal cancer. In future, we will explore further to investigate the mechanism of anticancer activity and clinical investigation of P-SLN. Keywords: Papain, cytotoxic potential, solid lipid nanoparticles, cell viability, proteolytic enzyme, Colorectal cancer (CRC).

Preparation, Thermophysical Studies, and Corrosion Analysis of a Stable Capric Acid/Cetyl Alcohol Binary Eutectic Phase Change Material for Cold Thermal Energy Storage

AbstractThis study focuses on the preparation, thermophysical properties, and corrosion analysis of a stable capric acid/cetyl alcohol eutectic phase‐change material (PCM) for application in the thermal comfort of buildings. Differential scanning calorimetry is used to investigate the thermal properties of the prepared eutectic PCM, and the results show that the eutectic composition of 70 % capric acid and 30 % cetyl alcohol was suitable for low‐temperature thermal energy storage as it had melting and freezing temperatures of 22.89 and 11.97 °C, respectively. The latent heats of melting and freezing of the eutectic PCM are 144.92 and 145.85 J g−1, respectively. The changes in the melting point and latent heat of the eutectic mixtures over continuous charging/discharging cycles are presented. The accelerated thermal cycling test and FTIR spectra show that the prepared eutectic PCM has a good thermal stability over 1000 thermal cycles. Moreover, corrosion compatibility tests for Cu, Al, and stainless steel 316 samples with the prepared eutectic PCM are discussed, and recommendations for the use of the PCM in the operational environment are presented.

Metronidazole-Loaded Polyethyleneimine and Chitosan-Based Liquid Crystalline System for Treatment of Staphylococcal Skin Infections.

Staphylococcus aureus is a common gram-positive bacterium of the human skin microbiota. It is also a dangerous pathogen that can cause serious and even lethal skin infections. The topical administration of metronidazole via nanotechnology-based drug delivery systems, such as liquid crystalline systems, can modulate both the drug permeation and activity, decreasing its side effects and increasing the drug potent activity against the gram-positive bacteria. This study aimed at: (1) structurally developing and characterizing a liquid crystalline systems composed of chitosan and polyethyleneimine dispersion as the aqueous phase, oleic acid as the oily phase, and ethoxylated and propoxylated cetyl alcohol as the surfactant (FPC) for metronidazole incorporation (0.5% w/w); (2) evaluating the in vitro release and skin permeation and retention properties of the metronidazole-loaded liquid crystalline systems (FPC-M); (3) investigating the in vitro antibacterial activity of FPC-M against Staphylococcus aureus. Polarised light microscopy indicated that both FPC and FPC-M are hexagonal systems. Rheological, texture, and bioadhesion assays showed that both are elastic and bioadhesive systems. According to the results of the in vitro release, permeation, and retention assays, FPC can modulate metronidazole release and allow metronidazole to stay for a longer time on the skin. The determination of FPC-M activity against Staphylococcus aureus showed that it could target the bacterial cell. In conclusion, the liquid crystalline systems developed in this study can improve the clinical performance of metronidazole in the treatment of staphylococcal skin infections.

A STABILITY INDICATING MICELLAR LIQUID CHROMATOGRAPHIC METHOD FOR THE DETERMINATION OF DEFERASIROX IN SOLUBILIZED SYSTEM

A simple, isocratic and stability indicating micellar liquid chromatographic (MLC) method containing a surfactant solution above its critical micellar concentration (CMC) was developed and validated for determination of Deferasirox (BTBA) content in active pharmaceutical ingredient and its pharmaceutical formulations. The analysis was performed in on isocratic mode at 400C temperature through Thermo Hypersil ODS 100mmA—4.6mm, 3 µm particle size columns. The UV detection wavelength was set at 250 nm in the mobile phase containing 0.1 M Cetyl trimethyl ammonium bromide (CTAB) buffer (pH – 2.5) and 10% 1-butanol. The method was successfully validated following as per the requirements of ICH guidelines. The proposed method was successfully applied as stability indicating method for determination of BTBA under different stressed conditions. The method allows accurate and reliable determination of BTBA for drug stability assay in pharmaceutical investigations.

Development and characterization of p1025-loaded bioadhesive liquid-crystalline system for the prevention of Streptococcus mutans biofilms.

Formation of a dental biofilm by Streptococcus mutans can cause dental caries, and remains a costly health problem worldwide. Recently, there has been a growing interest in the use of peptidic drugs, such as peptide p1025, analogous to the fragments 1025–1044 of S. mutans cellular adhesin, responsible for the adhesion and formation of dental biofilm. However, peptides have physicochemical characteristics that may affect their biological action, limiting their clinical performance. Therefore, drug-delivery systems, such as a bioadhesive liquid-crystalline system (LCS), may be attractive strategies for peptide delivery. Potentiation of the action of LCS can be achieved with the use of bioadhesive polymers to prolong their residence on the teeth. In line with this, three formulations – polyoxypropylene-(5)-polyoxyethylene-(20)-cetyl alcohol, oleic acid, and Carbopol C974P in different combinations (F1C, F2C, and F3C) were developed to observe the influence of water in the LCS, with the aim of achieving in situ gelling in the oral environment. These formulations were assessed by polarized light microscopy, small-angle X-ray scattering, rheological analysis, and in vitro bioadhesion analysis. Then, p1025 and a control (chlorhexidine) were incorporated into the aqueous phase of the formulation (F + p1025 and F + chlorhexidine), to determine their antibiofilm effect and toxicity on epithelial cells. Polarized light microscopy and small-angle X-ray scattering showed that F1C and F2C were LCS, whereas F3C was a microemulsion. F1C and F2C showed pseudoplastic behavior and F3C Newtonian behavior. F1C showed the highest elastic and bioadhesive characteristics compared to other formulations. Antibiofilm effects were observed for F + p1025 when applied in the surface-bound salivary phase. The p1025-loaded nanostructured LCS presented limited cytotoxicity and effectively reduced S. mutans biofilm formation, and could be a promising p1025-delivery strategy to prevent the formation of S. mutans dental biofilm.

Single Layer Extended Release Two-in-One Guaifenesin Matrix Tablet: Formulation Method, Optimization, Release Kinetics Evaluation and Its Comparison with Mucinex® Using Box-Behnken Design.

Guaifenesin, a highly water-soluble active (50 mg/mL), classified as a BCS class I drug. Owing to its poor flowability and compressibility, formulating tablets especially high-dose one, may be a challenge. Direct compression may not be feasible. Bilayer tablet technology applied to Mucinex®, endures challenges to deliver a robust formulation. To overcome challenges involved in bilayer-tablet manufacturing and powder compressibility, an optimized single layer tablet prepared by a binary mixture (Two-in-one), mimicking the dual drug release character of Mucinex® was purposed. A 3-factor, 3-level Box-Behnken design was applied to optimize seven considered dependent variables (Release "%" in 1, 2, 4, 6, 8, 10 and 12 h) regarding different levels of independent one (X1: Cetyl alcohol, X2: Starch 1500®, X3: HPMC K100M amounts). Two granule portions were prepared using melt and wet granulations, blended together prior to compression. An optimum formulation was obtained (X1: 37.10, X2: 2, X3: 42.49 mg). Desirability function was 0.616. F2 and f1 between release profiles of Mucinex® and the optimum formulation were 74 and 3, respectively. An n-value of about 0.5 for both optimum and Mucinex® formulations showed diffusion (Fickian) control mechanism. However, HPMC K100M rise in 70 mg accompanied cetyl alcohol rise in 60 mg led to first order kinetic (n = 0.6962). The K values of 1.56 represented an identical burst drug releases. Cetyl alcohol and starch 1500® modulated guaifenesin release from HPMC K100M matrices, while due to their binding properties, improved its poor flowability and compressibility, too.