Commercial Formulations Research Articles

Synergistic anticancer effects and reduced genotoxicity of silver nanoparticles and tamoxifen in breast cancer cells

AbstractNanotechnology is emerging as a promising tool to enhance traditional cancer treatments due to rising chemotherapy resistance and the severe side effects of toxic drugs. Silver nanoparticles (AgNPs) are widely acknowledged for their antimicrobial and antiproliferative properties. Given these AgNP characteristics, this research conducts a comprehensive nanotoxicological assessment of strategic combinations involving AgNPs (68 nm) commercial formulation and tamoxifen on MCF‐7 and MDA‐MB‐231 breast tumor cells. Utilizing CompuSyn software, the combination index was determined, revealing a synergistic cytotoxic and antiproliferative effect in AgNPs and tamoxifen combinations (CI < 0.97). Furthermore, this combination impaired cell migration (the scratch zone expanded by over 270%) and significantly increased reactive oxygen species production (up to 96% for MDA‐MB‐231 and 52% for MCF‐7 cells). Surprisingly, the genotoxic effect of these mixtures was minimal (below the allowable genotoxicity index of 1.5). Additionally, both breast tumor cell lines exhibited increased proapoptotic and oxidative stress gene expression following the combined treatment. The internalization of AgNPs into breast cancer cells was observed, enhancing their synergistic antiproliferative effect when combined with tamoxifen. These findings suggest the potential of combining AgNPs with chemotherapeutic agents for innovative studies in oncology therapy.

Overview of human health effects related to glyphosate exposure.

Glyphosate is a chemical compound derived from glycine, marketed as a broad-spectrum herbicide, and represents one of the most widely used pesticides in the world. For a long time, it was assumed that glyphosate was harmless, either due to its selective enzymatic acting method on plants, and because commercial formulations were believed to contain only inert chemicals. Glyphosate is widely spread in the environment, the general population is daily exposed to it via different routes, including the consumption of both plant, and non-plant based foods. Glyphosate has been detected in high amounts in workers' urine, but has been detected likewise in bodily fluids, such as blood and maternal milk, and also in 60%-80% of general population, including children. Considering its massive presence, daily exposure to glyphosate could be considered a health risk for humans. Indeed, in 2015, the IARC (International Agency for Research on Cancer) classified glyphosate and its derivatives in Group 2A, as probable human carcinogens. In 2022, nevertheless, EFSA (European Food Safety Authority) stated that the available data did not provide sufficient evidence to prove the mutagenic/carcinogenic effects of glyphosate. Therefore, the European Commission (EC) decided to renew the approval of glyphosate for another 10years. The purpose of this review is to examine the scientific literature, focusing on potential risks to human health arising from exposure to glyphosate, its metabolites and its commercial products (e.g., Roundup®), with particular regard to its mutagenic and carcinogenic potential and its effects as endocrine disrupter (ED) especially in the human reproductive system.

Amorphous Solid Dispersion Formation for Enhanced Release Performance of Racemic and Enantiopure Praziquantel.

Praziquantel (PZQ) is the treatment of choice for schistosomiasis, which affects more than 250 million people globally. Commercial tablets contain the crystalline racemic compound (RS-PZQ) which limits drug dissolution and oral bioavailability and can lead to unwanted side effects and poor patient compliance due to the presence of the S-enantiomer. While many approaches have been explored for improving PZQ's dissolution and oral bioavailability, studies focusing on investigating its release from amorphous solid dispersions (ASDs) have been limited. In this work, nucleation induction time experiments were performed to identify suitable polymers for preparing ASDs using RS-PZQ and R-PZQ, the therapeutically active enantiomer. Cellulose-based polymers, hydroxypropyl methylcellulose acetate succinate (HPMCAS, MF grade) and hydroxypropyl methylcellulose (HPMC, E5 LV grade), were the best crystallization inhibitors for RS-PZQ in aqueous media and were selected for ASD preparation using solvent evaporation (SE) and hot-melt extrusion (HME). ASDs prepared experimentally were subjected to X-ray powder diffraction to verify their amorphous nature and a selected number of ASDs were monitored and found to remain physically stable following several months of storage under accelerated-stability testing conditions. SE HPMCAS-MF ASDs of RS-PZQ and R-PZQ showed faster release than HPMC E5 LV ASDs and maintained good performance with an increase in drug loading (DL). HME ASDs of RS-PZQ formulated using HPMCAS-MF exhibited slightly enhanced release compared to that of SE ASDs. SE HPMCAS-MF ASDs showed a maximum release increase of the order of 6 times compared to generic and branded (Biltricide) PZQ tablets. More importantly, SE R-PZQ ASDs with HPMCAS-MF released the drug as effectively as RS-PZQ or better, depending on the DL used. These findings have significant implications for the development of commercial PZQ formulations comprised solely of the R-enantiomer, which can result in mitigation of the biopharmaceutical and compliance issues associated with current commercial tablets.

Method Development and Stress Degradation Profile of Umifenovir by UV Spectrophotometry

A simple, selective, and economical UV spectrophotometric method has been developed using ethanol as solvent (50%) to determine the umifenovir content in bulk and pharmaceutical dosage formulations. At a pre-determined λ max of 260 nm, it has shown linear in the 10-50 µg/mL range and exhibited a good correlation coefficient (R2 = 0.9927) and excellent mean recovery (98.00–104%). The method was validated statistically, and recovery studies were done for linearity, precision, and accuracy. The obtained results proved that the method can be employed for the routine analysis of umifenovir in bulks and commercial formulations. Keywords: UV spectrophotometry, Umifenovir, Validation, Method development, Stress Degradation

Acute toxicity of chlorpyrifos to some non-target freshwater organisms: which one is more toxic-technical grade or commercial formulation?

Chlorpyrifos is among the most widely sold organophosphates in the agriculture sector worldwide. Static bioassays were performed in the laboratory to compare the acute toxicity between the technical grade (94% a.i.) and commercial formulation (20% EC) of chlorpyrifos to four freshwater organisms: the crustacean zooplankton Cyclops viridis, the oligochaete worm Branchiura sowerbyi, the gastropod Pila globosa, and tadpole larvae of Duttaphrynus melanostictus. The recovery of actual chlorpyrifos concentrations in water after 2 h of exposure to the nominal concentrations ranged from 82.98% to 88.56%. The commercial formulation (F) of chlorpyrifos was found to be 1.94 to 2.76 times more toxic than the technical grade (T). Based on 96 h LC50 values of T and F chlorpyrifos, C. viridis was found to be most sensitive (0.56 and 0.25 μg/L) and P. globosa as most tolerant (1482 and 536 μg/L) to chlorpyrifos. Changes in LC50 values of both T and F chlorpyrifos were noted in respect of exposure hours for the three aquatic invertebrates and the tadpole larvae of the toad. In conclusion, the acute toxicity of chlorpyrifos to some non-target freshwater organisms differs between technical grade and commercial formulations.

Exploring Hydrogel Nanoparticle Systems for Enhanced Ocular Drug Delivery.

Drug delivery to the ocular system is affected by anatomical factors like the corneal epithelium, blinking reflex, aqueous blood barrier, and retinal blood barrier, which lead to quick removal from the site and inefficient drug delivery. Developing a drug delivery mechanism that targets specific eye tissue is a major hurdle for researchers. Our study examines the challenges of drug absorption in these pathways. Hydrogels have been researched as a suitable delivery method to overcome some obstacles. These are developed alone or in conjunction with other technologies, such as nanoparticles. Many polymer hydrogel nanoparticle systems utilizing both natural and synthetic polymers have been created and investigated; each has pros and cons. The complex release mechanism of encapsulated agents from hydrogel nanoparticles depends on three key factors: hydrogel matrix swelling, drug-matrix chemical interactions, and drug diffusion. This mechanism exists regardless of the type of polymer. This study provides an overview of the classification of hydrogels, release mechanisms, and the role of controlled release systems in pharmaceutical applications. Additionally, it highlights the integration of nanotechnology in ocular disease therapy, focusing on different types of nanoparticles, including nanosuspensions, nanoemulsions, and pharmaceutical nanoparticles. Finally, the review discusses current commercial formulations for ocular drug delivery and recent advancements in non-invasive techniques. The objective is to present a comprehensive overview of the possibilities for enhancing ocular medication delivery through hydrogel nanoparticle systems.

Selecting Bacillus strains antagonist to Erysiphe necator (Schw.) Burr. the causal agent of grape powdery mildew

ABSTRACT Grape powdery mildew (GPM) control is based on the preventive use of sulfur and curative application of synthetic fungicides, increasing the risk for producers’ health and environmental and fruit contamination. This work aimed to select Bacillus strains isolated from the Brazilian tropical semi-arid region that are effective antagonists to GPM. In an initial screening performed by spraying bacterial suspensions in detached grape leaves, six strains of Bacillus spp. showed disease symptom reduction higher than 70.0%. Two greenhouse experiments showed that the bacterial strains LCB03, LCB28, and LCB30 showed control efficiency >80%, statistically similar to a commercial formulation with Bacillus amyloliquefaciens QST713. 16s rDNA sequencing showed that strain LCB03 showed 100.0% homology to B. velezensis, while LCB28 has high homology to B. tequillensis (99.93%), and LCB30 had 99.71% homology with B. siamensis. As an average for both greenhouse experiments, weekly application of Bacillus sp LCB03, Bacillus sp LCB28, and Bacillus sp. LCB30 reduced the average incidence by around 50% and more than 80% for GPM severity.

Development of leaf-adhesive polyurethane microcapsules loaded with prochloraz for enhanced fungicide efficiency

Leaf-adhesive pesticide microcapsules represent a promising approach to improving pesticide efficacy while minimizing environmental pollution. In this study, we developed a leaf-adhesive polyurethane microcapsule loaded with prochloraz (Pro@CS-OP-10) using a reactive emulsifier (OP-10) via interfacial polymerization. Physicochemical analysis revealed microcapsules with smooth surfaces and uniform distribution, averaging 1.97 μm in size, with an encapsulation efficiency of 96.38 %. Comparative assessments demonstrated superior wetting and adhesion properties of Pro@CS-OP-10 on wheat leaves compared to other commercial formulations. Moreover, the polyurethane shell effectively enhanced the photostability of encapsulated prochloraz and hindered its rapid release. Fungal growth rate experiments indicated prolonged inhibitory effects of Pro@CS-OP-10 on Fusarium graminearum, with median inhibitory concentrations (EC50) on the second and eighth day being 0.018 mg/L and 0.045 mg/L. Therefore, the leaf-adhesive Pro@CS-OP-10 shows great potential as an environmentally friendly fungicidal formulation.

A novel pesticide has lethal consequences for an important pollinator

Wild bees pollinate crops and wildflowers where they are frequently exposed to pesticides. Neonicotinoids are the most commonly used insecticide globally, but restrictions on their use and rising pest resistance have increased the demand for alternative pesticides. Flupyradifurone is a novel insecticide that has been licenced globally for use on bee-visited crops. Here, in a semi-field experiment, we exposed solitary bees (Osmia lignaria) to a commercial pesticide formulation (Sivanto Prime) containing flupyradifurone at label-recommended rates. We originally designed the experiment to examine sublethal effects, but contrary to our expectations, 100 % of bees released into pesticide-treated cages died within 3 days of exposure, compared to 0 % in control plots. Bees exposed to flupyradifurone a few days after the initial application survived but endured prolonged sublethal effects, including lower nesting success, impairment to foraging efficiency, and higher mortality. These results demonstrate that exposure to this novel insecticide poses significant threats to solitary bees and add to a growing body of evidence indicating that this pesticide can have negative impacts on wild bees at field-realistic concentrations. In the short-term, we recommend that commercial formulations containing flupyradifurone should be restricted to non-flowering crops while a reassessment of its safety can be conducted. In the long-term, environmental risk assessors should continue to develop risk assessments that are truly holistic and incorporate the ecological and life history traits of multiple pollinator species.

A novel QbD HPLC approach for the concurrent analysis of amoxicillin, amprolium, and ethopabate in food samples and dosage forms

A simple, rapid, and sensitive reversed-phase HPLC method coupled with photodiode array detection (PDA) was developed for the simultaneous estimation of three co-administered antibacterial drugs, amprolium, ethopabate, and amoxicillin for the first time. An analytical quality-by-design (QbD) approach was adopted to optimize the developed approach. A two-level full factorial design (25 FFD) was implemented to optimize how variable factors affected chromatographic responses. On a Hypersil BDS C18 column, the chromatographic separation was carried out using isocratic elution at 40.1 °C. The mobile phase consisted of methanol: potassium phosphate buffer containing 5.76 mM heptane sulphonate (9.05 mM; pH 3.32, 44.8:55.2 % v/v) pumped at a flow rate of 0.8 mL/min and an injection volume of 20.0 μL. In less than 7 min, the suggested method was able to separate the ternary mixture with a challenging ratio of 1: 15.6: 1 for amoxicillin, amprolium, and ethopabate, respectively. The calibration curves showed excellent linearity over the concentration ranges of 0.50–30.0, 0.30–30.0, and 0.05–20.0 μg/mL, respectively. Recovery percentages ranged from 90.30 % to 111.13 % with %RSD less than 2 % were obtained upon spiking to chicken tissues, liver, and egg samples, indicating the suitability of the proposed method for determining of the studied drugs in complicated food matrices. Furthermore, the proposed method was successfully applied to determine the studied drugs in their commercial formulations. Full validation was carried out according to ICHQ2 (R1) guidelines. Finally, the method's greenness and ecofriendliness were evaluated using various metrics tools, including the Green Analytical Procedure Index (GAPI) and Analytical GREEnness (AGREE).

Novel insights into the photochemical transformation of neonicotinoid insecticides: Potential involvement of adjuvants

Commercial pesticide formulations often contain both the active ingredient and different adjuvants, the potential impacts of adjuvants on pesticides’ transformation have been barely considered. In this study, effects of typical adjuvants (i.e. hexadecyl trimethyl ammonium bromide (CTAB), hexadecyl trimethyl ammonium chloride (CTAC) and p-Octyl polyethylene glycol phenyl ether (TX-100)) on the photodegradation of four selected neonicotinoid insecticides (NIs), including thiamethoxam (TMX), dinotefuran (DIN), imidacloprid (IMP) and acetamiprid (ACP) were systematically investigated. Specifically, CTAB and CTAC exhibited minimal or no impact on the photolysis of four NIs, while TX-100 significantly inhibited their decay. Such inhibitory effect could mainly be attributed weakening the formation of key transient intermediates, such as the corresponding radical cation (NI•+), radical anion (NI•-) as well as hydrated electron (eaq-). Photoproducts identification revealed a novel transformation pathway of NIs in the presence of TX-100, characterized by de-chain reactions, resulting in the formation of photostable dimeric photoproducts. These dimers exhibited varying toxicity: for TMX, DIN and IMP, their corresponding dimers showed increased toxicity compared to their parent compounds, whereas for ACP, they displayed decreased toxicity. These provide important information for the evaluation the environmental fates and toxicology of formulaic NIs.

Decoration of recycled battery graphite functionalized with gold nanoparticles/poly(nicotinic acid) for detection of bifenazate pesticide in tea and food samples

Bifenazate (BF), is a type of carbamate acaricide effective at controlling mite parasites on crops and ornamental plants. In this work, a recycled dry zinc-carbon battery graphite electrode decorated with gold nano particles/poly nicotinic acid, AuNPs/poly(NA)-BGE, was applied as the working electrode for the electrochemical measurement of bifenazate (BF). The working electrode (BGE) was functionalized by 10 electropolymerization voltammetric cycles of poly nicotinic acid poly (NA) following by 30 s of amperometric deposition of gold nanoparticles (AuNPs) to produce the final AuNPs/poly(NA)-BGE electrode in a two-step procedure. “Electrochemical and morphological characterization of the sensor at its different production steps was performed using electrochemical impedance spectroscopy (EIS), cyclic voltammetry (CV), scanning electron microscopy (SEM), atomic force microscopy (AFM), energy dispersive X-ray spectroscopy (EDX) techniques and Transmission electron microscopy (TEM).” The highest peak current response was attained using pH 6.0 in 0.1 M phosphate buffer. The sensor exhibited a linearity range from (1 × 10−4–1 × 10−8 M) that is equivalent to 30.035–3.00 × 10−3 µg/mL with limits of detection LOD and quantification 3.3 × 10−11 M (9.91 × 10−6 µg/mL) and 1.00 × 10−10 M (3.00 × 10−5 µg/mL), respectively. Finally, with a recovery range of (96.3 %–102.6 %) and an RSD of (0.17 %–0.64 %), BF in Kenyan green and black tea, strawberry, tomato, cucumber and its commercial formulation Duramite® 24 %SC was successfully quantified which indicates the promising applicability of the presented sensor in different matrixes.

Physiological responses of the stingless bee Partamona helleri to oral exposure to three agrochemicals: impact on antioxidant enzymes and hemocyte count.

Agrochemicals pose significant threats to the survival of bees, yet the physiological impacts of sublethal doses on stingless bees remain poorly understood. This study investigated the effects of acute oral exposure to three commercial formulations of agrochemicals [CuSO4 (leaf fertilizer), glyphosate (herbicide), and spinosad (bioinsecticide)] on antioxidant enzymes, malondialdehyde content (MDA), nitric oxide (NO) levels, and total hemocyte count (THC) in the stingless bee Partamona helleri. Foragers were exposed to lethal concentrations aimed to kill 5% (LC5) of CuSO4 (120μgmL-1) or spinosad (0.85μgmL-1) over a 24-h period. Glyphosate-exposed bees received the recommended label concentration (7400μgmL-1), as they exhibited 100% survival after exposure. Ingestion of CuSO4 or glyphosate-treated diets by bees was reduced. Levels of NO and catalase (CAT) remained unaffected at 0h or 24h post-exposure. Superoxide dismutase (SOD) activity was higher at 0h compared to 24h, although insignificantly so when compared to the control. Exposure to CuSO4 reduced glutathione S-transferase (GST) activity at 0h but increased it after 24h, for both CuSO4 and glyphosate. MDA levels decreased after 0h exposure to CuSO4 or spinosad but increased after 24h exposure to all tested agrochemicals. THC showed no difference among glyphosate or spinosad compared to the control or across time. However, CuSO4 exposure significantly increased THC. These findings shed light on the physiological responses of stingless bees to agrochemicals, crucial for understanding their overall health.

Trichoderma role as an essential plant growth promotion-a review

In the world, pest infestation is responsible for 70% or more of per cent losses in agricultural productivity, and mycopesticide can provide an alternative option to pest control option as an alternative to synthetic pesticides. Trichoderma is a genus of fungal species, and Trichoderma viride is one of the known fungal species in categories that exhibit biocontrol mechanisms since it is well-identified for 100% effectiveness in pest control. The mycelium of T. viride has shown its capabilities for the production of various types of enzymes, including cellulases and chitinase, with degradation capability for celluloses and chitin polymers, respectively. It is ubiquitous in nature. It is widely used for the management of crop diseases and is basically soil-borne, but it is also foliar. Trichoderma has shown its potential due to diversity, ecology, and application. The mechanism of action includes competition, production of different metabolites, induced resistance and enzymes, etc. There are several commercial formulations available all over the world that are used against crop diseases. Trichoderma, due to its potential for degradation capability, can be utilised from waste to wealth. Later on, with the development of more research on Trichoderma, various utilities were found. This includes its effective control against harmful insects in agricultural as well as health sectors. It also can detoxify the heavy metals. In the health sector, continuous exploration of its benefits for drug discovery is being done. As a whole, it can be considered soil gold and a promising future beneficial microbe.

Imaging-Based Drug Penetration Profiling in an Excised Sheep Cornea Model.

Formulations designed to address ocular conditions and diseases are predominantly administered topically. While in vitro test systems have been developed to assess corneal permeation under extended contact conditions, methods focusing on determining the penetration depth and kinetics of a substance within the cornea itself rather than through it, are scarce. This study introduces a method for time-dependent penetration depth analysis (10 and 60 min) by means of a semiquantitative imaging method in comparison with a quantitative corneal depth-cut technique, employing fluorescein sodium at concentrations of 0.2 and 0.4 mg/mL as a small molecule model substance and sheep cornea as a human surrogate. Excised tissues exhibited sustained viability in modified artificial aqueous humor and maintained thickness (746 ± 43 µm) and integrity (electrical resistance 488 ± 218 Ω∙cm2) under the experimental conditions. Both methods effectively demonstrated the expected concentration- and time-dependent depth of penetration of fluorescein sodium, displaying a significantly strong correlation. The traceability of the kinetic processes was validated with polysorbate 80, which acted as a penetration enhancer. Furthermore, the imaging-based method enabled detecting the retention of larger structures, such as hyaluronic acid and nanoemulsions from the commercial eyedrop formulation NEOVIS® TOTAL multi, inside the lacrimal layer.

Ex-vivo skin retention of crisaborole from microemulsion and micellar formulations

The aim of the present work was to optimize the delivery of crisaborole to the skin, incorporating the drug in topical formulations with a texture suitable also for application to the hairy skin. In particular we focused on microemulsions and micelles. As reference, the concentration of crisaborole in skin layers obtained with the commercial ointment Eucrisa®, was considered. Two microemulsions, one w/o and one o/w, were tested ex-vivo and both produced drug deposition into the skin comparable to the commercial formulation, but with higher delivery efficiency and with a non measurable permeation across the skin. Solutol®, TPGS and Soluplus® at different concentration were used for the preparation of crisaborole micellar solutions. Compared to the commercial formulation, all the micellar systems produced lower drug concentration in the skin layers, with the only exception of Soluplus® 6 %. However, due to differences in drug loading and thus in the applied dose, the delivery efficiency of all the formulation tested was higher compared to the commercial ointment. Moreover with Soluplus® 6 % formulation, a 5-fold increase in the retained/permeated ratio compared to the ointment was obtained. Two-photon microscopy studies showed that Soluplus® 6 % micelles do not permeate intact across the skin but disassemble in correspondence of the tissue surface.

Dual-stimuli-responsive silica-based emamectin benzoate nanodelivery system for effective control of Spodoptera frugiperda and safety assessment toward Microplitis manilae

The utilization of highly efficient and ecofriendly stimulus-responsive delivery systems for pesticides represents a powerful strategy for enhancing their efficacy and environmental safety. In this study, the application of emamectin benzoate (EB)-loaded amino-functionalized rough mesoporous silica (KMSNs)@poly(glycidyl methacrylate-co-acrylic acid) (PMA) composites (KMSNs@PMA@EB, 6.52 % loading capacity for EB) to control efficacy for Spodoptera frugiperda was investigated in detail. The results showed that, KMSNs@PMA@EB rapidly released EB under acidic and high-temperature conditions. compared with EB and commercial formulations, a solution of KMSNs@PMA@EB with the agricultural organosilicon additive exhibited excellent wetting. Compared with MSNs, KMSNs@PMA significantly enhanced the effective deposition. Moreover, the photostability of KMSNs@PMA@EB was improved by 1.87-fold and 2.25-fold compared to EB and an EB suspension concentrate (EB SC). S. frugiperda larvae preferred corn leaves with low concentrations (0.125 mg/L) of KMSNs@PMA@EB than EB-treated. Bioassays revealed that KMSNs@PMA@EB maintained > 37 % control efficiency after 21 d of spraying, KMSNs@PMA@EB exhibited significantly greater insecticidal activity and persistence against S. frugiperda than commercial formulations. After 21 days of application, the final deposition rates of KMSNs@PMA@EB were lower than the maximum residual limit of EB, spraying KMSNs@PMA@EB has a lower impact on corn plants. Furthermore, biological safety assessments confirmed that KMSNs@PMA@EB did not affect the maize seed germination and growth and posed a low risk to Microplitis manilae. Those results highlight that the advantages of KMSNs@PMA@EB nanoparticles multidimensional enhancement of pesticide efficacy, persistence, and safety to parasitic wasps and has great potential to be used in pest control combining parasitoid and nanopesticides.

The Development and Pre-Clinical Anti-Inflammatory Efficacy of a New Transdermal Ureasil-Polyether Hybrid Matrix Loaded with Flavonoid-Rich Annona muricata Leaf Extract.

This study aimed to develop a novel ureasil-polyether transdermal hybrid matrix (U-PEO) loaded with Annona muricata concentrated extract (AMCE), which exhibits potent anti-inflammatory activity. The extract was obtained by maceration, a method that allowed for the extraction of a high concentration of flavonoids (39.27 mg/g of extract). In vivo tests demonstrated that 10 mg/kg of AMCE inhibited inflammation for 6 h. The physicochemical characterization of U-PEO with AMCE was conducted via a thermogravimetric analysis (TGA), while its surface was recorded using atomic force microscopy (AFM). The in vitro macroscopic swelling and release tests demonstrated the hydrophilic profile of the material and the percentage of AMCE released. The TGA results demonstrated that the system exhibited physical compatibility due to the thermal stability of U-PEO. Additionally, the AFM analysis revealed a rough and porous surface, with a particular emphasis on the system with AMCE. The release resulted in the liberation of 23.72% of AMCE within 24 h. Finally, the preclinical tests demonstrated that U-PEO with AMCE was also capable of effectively inhibiting inflammation for 6 h, a duration comparable to that of a commercial formulation. The results permit the advancement of the study towards the development of a transdermal system, thereby rendering its application in clinical studies feasible.

Harnessing a thermo-active and alkaline lipase from novel strain of Brevibacillus borstelensis gp-1, for application in biodiesel synthesis

A novel thermo-active and alkaliphilic strain of Gp-1, isolated from hot water springs of Ganeshpuri, Maharashtra, India, identified as Brevibacillus borstelensis based on 16SrDNA characterization, with accession no. MT292327, at NCBI database. Statistical optimization of lipase production was done using Plackett-Burman algorithm and response surface methodology. Fermentative production of Gp-1 lipase was followed by partial purification, with 24.10 fold purification. Gp-1 lipase has molecular mass of 31 kDa, as determined by SDS-PAGE. Gp-1 lipase exhibited maximal specific activity at pH 10 and 55 °C, with stability up to 70 °C. Kinetic parameters analysis revealed Gp-1 lipase has Km and Vmax values of 1.544 mM and 31.25 μM/mg. min, and specificity constant of 281.13 sec-1, with pNP caprylate as the base suited substrate. Gp-1 lipase was found to be retain more than 90% activity in presence of various organic solvents, and various commercial detergent formulations. The Gp-1 lipase was also tested for transesterification reactions, which revealed successful transesterification of coconut oil, olive oil and waste cooking oil, and conversion in esters. Hence, Gp-1 lipase stands out as a prospective candidate in biodiesel synthesis, a green energy alternative.

Enhancement of Solubility and Dissolution Rate of Simvastatin Tablets by Liquisolid Compact Approach

The aim of the current work was to improve the solubility and dissolution rate of poorly water-soluble drug, simvastatin (SM) by using the liquisolid compact technique (LS; SM-LS). Liquid load factors, and excipient ratios were used to calculate the required amounts of excipients necessary to prepare the SM-LS and compressed to tablets according to mathematical models. Avicel PH102, Aerosil 200 and Crosspovidone (CP) was used as carrier, coating material and disintegrant, respectively. Drug-excipient mixtures were evaluated compatibility by Attenuated total reflectance (ATR) and differential scanning calorimetry (DSC). Prepared SM-LS formulations were evaluated for various pre-compression and post-compressional parameters, in-vitro dissolution, and stability studies (40 ± 2°C / 75 ± 5% RH) for 3 months. Among the different formulations, LS10 formulation which contains 30% drug, 5% CP, Avicel pH 102: Aerosil 200 (1:10) showed 14-folds increase in dissolution rate when compared with pure SM powder. FTIR-ATR and DSC studies confirmed that there was no interaction between the drug and excipients. Further, the LS10 formulation had shown comparable dissolution profile with commercially available tablet formulation. The LS10 formulation showed no significant changes in the physicochemical properties over 3 months during stability studies. Therefore, the SM loaded LS formulation could be considered as an alternative approach to enhance the solubility and dissolution for commercial formulations. Keywords: Liquisolids compacts, solubility, dissolution, carrier, coating material, stability.