Accelerated Storage Conditions Research Articles

Effects of physical refining process on quality and stability of argan oil (Argania Spinosa (L.) Skeels)

Subquality argan kernels are 30% cheaper than the regular kernels mandatory used to prepare edible argan oil. The use of these argan kernels for the preparation of argan oil intended to be a cosmetic ingredient, after bleaching and deodorization, is therefore particularly economically appealing. The oxidative stability of Argan oil prepared from subquality kernels is unknown. It was evaluated over a period of storage of 12 weeks at 60 °C, then compared with that of argan oil stored under the same conditions and originating from the same initial batch, but which had subsequently been simply bleached and deodorized (physical refining). Physical refining led to an increase in initial oil quality due the loss of free fatty acids (up to 30% for refined argan oil), primary and secondary oxidation products but also to a dramatic decrease of the oxidative stability of argan oil caused by the loss of tocopherols, witnessed by the up to 94% loss after 12 weeks under accelerated storage conditions. As a conclusion, the oxidative stability of argan oil prepared from subquality argan kernels remains difficult to be adequately and efficiently evaluated since the initial quality of the argan kernels is the subject of great variations.

Novel drug-drug co-amorphous systems of olaparib with nonsteroidal anti-inflammatory drugs with improved solubility, physical stability, antitumor activity and pharmacokinetics

Olaparib (OLA), the first FDA-approved PARP inhibitor, has been approved successively for monotherapy or maintenance treatment of ovarian, breast and pancreatic cancer. Unfortunately, the poor solubility and bioavailability of OLA have limited its application. In this study, novel drug-drug co-amorphous systems of OLA with five nonsteroidal anti-inflammatory drugs (NSAIDs), including flurbiprofen (FLU), ketoprofen (KET), ibuprofen (IBU), diclofenac (DIC) or indomethacin (IND), were prepared for improving the aqueous solubility of OLA and achieving combination therapy against ovarian cancer. These new co-amorphous products were confirmed by powder X-ray diffraction, differential scanning calorimetry, and Fourier transform infrared spectroscopy. Five co-amorphous systems were more soluble and released faster than the crystalline OLA in pH 6.8 buffer, and OLA-DIC and OLA-IND showed superior physicochemical stability under accelerated storage conditions. The antitumor activities of OLA-FLU, OLA-KET, OLA-IBU and OLA-DIC against OVCAR3 cell line were approximately increased by 3.5, 2.4, 2.7, and 6.0-fold than that of OLA, respectively. Moreover, pharmacokinetic studies of co-amorphous OLA-DIC in rats revealed that the OLA exhibited 6.14-fold improvement in AUC0-t value compared with crystalline OLA. Therefore, our study suggested that OLA-NSAIDs co-amorphous systems showed the great potentials to improve the solubility, dissolution behaviors, and bio-pharmaceutical performance of OLA.

Understanding Excipient-Induced Crystallization of Spray-Dried Amorphous Solid Dispersion

This study investigates the compatibility of excipients with the model system SDI-X and their role in the induced crystallization of the amorphous compound-X in tablet formulations. We aimed to establish a straightforward and practical screening approach for evaluating excipient-induced crystallization of SDI in tablet matrices. Three methodologies—binary powder mixture, binary compact, and bilayer tablets—were employed to qualitatively and quantitatively evaluate the recrystallization of SDI-X with various excipients under accelerated storage conditions. The results demonstrated that binary compacts, providing direct physical contact between SDI-X and excipients, are superior in reflecting realistic drug-excipient contact within pharmaceutical tablets, enabling a more accurate assessment of excipient-induced crystallization for SDI-X. In contrast, the broadly used conventional binary blends can significantly underestimate this risk due to insufficient proximity. In addition, the bilayer tablets further confirmed that crystallization initiates at the contact surface between SDI-X and the excipients. The study highlighted that not only hygroscopicity but also the type of excipient and its physical contact with SDI-X significantly influence the recrystallization extent and rate of SDI-X. Interestingly, less hygroscopic diluents such as mannitol and lactose induced much higher levels of crystallization of SDIs, contrary to expectations based on moisture content alone. This suggests that the excipient type and contact surface are more critical in inducing recrystallization than just the level of moisture. The findings emphasize the need for careful excipient selection, study design, and sample preparation to enable appropriate assessments of SDI-excipient compatibility.

Development and characterization of transdermal drug delivery system of ramosetron HCL using different polymers and their effect on In-vitro release

Transdermal Drug Delivery Systems (TDDS) offer a controlled and consistent release of medications, bypassing first-pass metabolism and minimizing side effects associated with traditional oral and intravenous therapies. This study focuses on the development and evaluation of Ramosetron HCl transdermal patches designed for sustained release to manage nausea and vomiting. Ramosetron HCl, a selective 5-HT₃ serotonin receptor antagonist, was incorporated into various formulations using different grades of Hydroxypropyl Methylcellulose (HPMC), Polyvinyl Pyrrolidone (PVP K30), and Polysorbate 80. The patches were prepared by solvent casting and evaluated for various parameters including thickness, weight variation, drug content, folding endurance, tensile strength, and in-vitro drug release. The calibration curve for Ramosetron HCl in 7.4 pH phosphate buffer was established with a λmax of 240 nm. Fourier Transform Infrared Spectroscopy (FTIR) was employed to ensure compatibility between the drug and excipients. Formulation F5 demonstrated optimal properties, including satisfactory drug release profiles and mechanical strength. Stability studies of F5 showed that the formulation maintained its release characteristics under accelerated storage conditions (40°C / 75% RH) for up to three months. This study confirms the potential of Ramosetron HCl transdermal patches as an effective alternative to oral dosage forms, providing sustained drug delivery and enhanced patient compliance.

Application of ATR-FTIR for Green Arabica Bean Shelf-Life Determination in Accelerated Storage.

Coffee bean oxidation is associated with enzymatic and non-enzymatic browning, the degradation of desirable aromatic compounds, the development of undesirable flavors, increased susceptibility to microbial spoilage, and volatile compound losses. This study investigated natural dry process (DP) and honey process (HP) green coffee beans stored in GrainPro® bags for 0, 5, 10, and 20 days under accelerated storage conditions at 30 °C, 40 °C, and 50 °C with relative humidity of 50%. A kinetic model was used to estimate the shelf life of the green coffee beans. DP recorded durability of 45.67, 29.9, and 24.92 days at 30 °C, 40 °C, and 50 °C, respectively, with HP 60.34, 38.07, and 19.22 days. Partial least squares (PLS) analysis was performed to build the models in order to predict the shelf life of coffee based on peroxide (PV) and thiobarbituric acid reactive substances (TBARS) values. In terms of prediction with leave-one-out cross-validation (LOOCV), PLS provided a higher accuracy for TBARS (R2 = 0.801), while PV was lower (R2 = 0.469). However, the auto-prediction showed good agreement among the observed and predicted values in both PV (R2 = 0.802) and TBARS (R2 = 0.932). Based on the variable importance of projection (VIP) scores, the ATR-FTIR peaks as 3000-2825, 2154-2150, 1780-1712, 1487-2483, 1186-1126, 1107-1097, and 1012-949 cm-1 were identified to be the most related to PV and TBARS on green coffee beans shelf life. ATR-FITR showed potential as a fast and accurate technique to evaluate the oxidation reaction that related to the loss of coffee quality during storage.

Ascorbic acid-enriched cactus mucilage coatings maintained quality attributes of roasted ‘Wichita’ pecan nuts under accelerated storage conditions

The potential of a cactus mucilage (CM)-based edible coating enriched with ascorbic acid (AA) for preserving microwave-roasted pecan nuts’ quality during accelerated storage was investigated. CM (3 %) was mixed with different concentrations of AA, which were 0.03, 0.015, and 0.09 %, to formulate edible coating solutions that were applied to microwave-roasted (700 W, 2.27 min) pecan nuts before accelerated storage for 25 days at 60 °C. Samples were taken at a 5-day interval to be analysed for colour properties (L = lightness, BI = browning index, and TCD = total colour difference), hardness, total yeast and mold, total flavonoids content (TFC), total phenolic content (TPC), ferric reducing antioxidant power (FRAP), DPPH radical scavenging activity, peroxidase (POD), and polyphenol oxidase (PPO) enzyme activities. Coating microwave-roasted pecan nuts with 3 % CM enriched with AA at low concentrations such as 0.015 % proved effective in preserving the colour, hardness, TPC, TFC, FRAP, and reducing the activities of POD and PPO enzymes. This study has demonstrated that CM enriched with AA edible coatings has the capacity to protect the quality and prolong the shelf-life of microwave-roasted pecan nuts.

Shelf Life Enhancement of Structured Lipids Rich in Omega-3 Fatty Acids Using Rosemary Extract: A Sustainable Approach.

This study investigates the efficacy of rosemary extract (RE) in stabilizing structured lipids (SL) developed using perilla seed oil (PSO) and palmolein (PO) under accelerated storage conditions. The oil samples, comprising PSO, Blend, and SL formulations with and without RE (1500 ppm) and BHT (200 ppm), were studied for their storage stability during a 30 day storage period at 65 °C, with the analysis carried out at 6 day intervals. Oxidative properties were comprehensively assessed, including both physical attributes (color, viscosity, and refractive index) and chemical parameters (peroxide value, free fatty acid (FFA), p-anisidine value, TOTOX value, conjugated dienes, and trienes). The results demonstrated that RE-enriched oil samples exhibited significantly higher oxidative stability (p < 0.05) compared to the control group. SL added with 1500 ppm of RE exhibited notable enhancements in quality parameters, showcasing reductions in FFA, TOTOX value, conjugated diene, and triene value by 44.01%, 35.42, 39.03, and 47.36, respectively, when compared to SL without any antioxidant. The RE at 1500 ppm concentration showed a similar effect as the synthetic antioxidant BHT at 200 ppm. Also, the RE demonstrated potent inhibition of the oxidation of polyunsaturated fatty acids, thereby contributing to the improved oxidative stability of the SLs. Furthermore, SL with RE also exhibited reduced degradation of the tocopherol content and total phenolic content during the storage period. Principal component analysis demonstrated that SL and blend followed similar oxidative characteristics as they fell within the same quadrant. These findings underscore RE as a potent source of antioxidants capable of scavenging free radicals and enhancing the oxidative stability of omega-3 fatty acid-rich SLs.

Uncertainty Degradation Model for Initiating Explosive Devices Based on Uncertain Differential Equations

The performance degradation of initiating explosive devices is influenced by various internal and external factors, leading to uncertainties in their reliability and lifetime predictions. This paper proposes an uncertain degradation model based on uncertain differential equations, utilizing the Liu process to characterize the volatility in degradation rates. The ignition delay time is selected as the primary performance parameter, and the uncertain distributions, expected values and confidence intervals are derived for the model. Moment estimation techniques are employed to estimate the unknown parameters within the model. A real data analysis of ignition delay times under accelerated storage conditions demonstrates the practical applicability of the proposed method.

Investigation of antioxidant edible coating and modified atmosphere packaging for enhancing storability of hazelnut kernels

This study investigated the effects of antioxidant edible coating and modified atmosphere packaging for improving storability of dried hazelnut kernels by delaying lipid oxidation and color degradation. Hazelnut kernels were coated with different coating matrix (methylcellulose and chitosan) that contain different antioxidant substances (DL-α-tocopherol acetate, cinnamon essential oil, rosemary essential oil and hazelnut oil) and subjected to an accelerated storage condition at 35 °C for 270 days. Hazelnut kernels were also packed under modified atmosphere (MAP) with 100 % N2 in mylar bags and stored at 35 °C for 180 days. Lipid oxidation (free fatty acids, K232 and K270, peroxide values) and color (browning index) were measured for investigating quality changes during the storage. The free fatty acids of kernels from two packaging experiments remained stable during storage. K232 value of MAP kernels was significantly lower (2.20) than that of control (2.90) at the end of the storage, showing delayed production of conjugated dienes. The chitosan based edible coating with encapsulated cinnamon essential oil and oleic acid (CH/ECO/OA) resulted in significantly (P < 0.05) lower PV values (0.53 meq/kg oil), and all the coated samples had the positive effect on reducing browning index with 12–25 compared with control. K270 (0.04–0.18) remained relatively low throughout the long-term storage. As a result, modified atmosphere packaging performed better than edible coatings. This study demonstrated the importance of implicating proper postharvest technology for reducing lipid oxidation and quality deteriorations of hazelnut kernels during prolonged storage.

Thermal oxidative stability and kinetics of lipophilic bioactive compounds degradation during accelerated storage of unroasted and roasted peanut oil

Due to the susceptibility of peanut lipids to autooxidation, which compromises food quality and safety, shelf-life studies are conducted. This research aimed to examine and compare the thermal oxidative stability of cold-pressed peanut oils (POs) from unroasted and roasted varieties (Virginia and Valencia) under accelerated storage conditions (60°C, in the dark) for 28 days. Degradation kinetics of phytonutrients and changes in the fatty acid profile, chemical oxidation indicators, and antioxidant activity were continuously monitored to assess the extent of oxidation. Results showed that acid, peroxide, and p-anisidine values, UV-spectrophotometric indexes, and total oxidation value increased in POs during storage with significant differences. Total tocopherols and phytosterols decreased with storage time, following a second-order kinetic model. After 28 days of storage, 25.5442.08% of phytosterols and 25.9248.17% of tocopherols were lost. The degradation rates of tocopherol were higher in roasted POs, while unroasted POs exhibited the highest rate of phytosterols degradation. Besides, there were slight differences in the fatty acid composition of all stored oils. In addition, all POs' DPPH radical inhibition decreased with storage time, reaching values between 35.72% and 44.73%. This study has provided important insights into the evolution of key chemical parameters of unroasted and roasted POs of two commercial varieties during storage.

Microbial shelf-life estimation of frozen crispy chicken curry puff under accelerated storage conditions

Microbial shelf-life estimation of frozen crispy chicken curry puff under accelerated storage conditions

Formulation Development and Evaluation of Montelukast Sodium Paper Tablets for Enhanced Drug Release

In this study, the technique of paper-based tablets was evaluated for solubility enhancement of montelukast sodium (MS), an anti-asthmatic, Biopharmaceutical Classification System (BCS) class II medication. Initially, the potential for compressing regular paper into tablets was rigorously examined. Results demonstrated that paper may be utilised to make tablets, regardless of type of the paper utilized. The medicinal quality was satisfactory; and entire tablets of the batch met the Indian Pharmacopeia’s criteria. Compressing drug-loaded paper resulted in the formation of drug-loaded tablets. The MS loaded tablets prepared using kitchen roll paper delivered the best results. The tablet was disintegrated in 27 seconds, and drug release of MS was enhanced by 1.88 folds. The tablets were sufficiently hard, and they did not get broken during friability studies. Also, the tablets passed the other evaluation parameters. These paper tablets were also stable under accelerated storage conditions.

Novel Pharmaceutical Cocrystals of Tegafur: Synthesis, Performance, and Theoretical Studies.

Tegafur (TF) is one of the most important clinical antitumor drugs with poor water solubility, severely reducing its bioavailability. This work develops new cocrystals to improve the solubility of TF and systematically investigates the intermolecular interactions to provide new insights into the formation of cocrystal and changes in physicochemical properties. In this paper, two new 1:1 cocrystals of TF with 2,4 dihydroxybenzoic acid (2,4HBA) and p-nitrophenol (PNP) were synthesized. The cocrystal products were identified and characterized by various solid state analysis techniques. And the high performance liquid chromatography (HPLC) was conducted to determine the solubility and dissolution rate of TF and cocrystals. Moreover, the quantum chemistry calculations of crystal structure provided theoretical support for the results. Compared with pure TF, the solubility and dissolution rate of TF-2,4HBA is significantly increased in a pH 6.8 buffer at 37°C. Under accelerated storage conditions (40°C, 75% RH), all cocrystal exhibits excellent stability over 8weeks. Hirshfeld surface (HS) analysis, atoms in molecules (AIM) analysis, interaction region indicator (IRI) analysis, molecular electrostatic potential surface (MEPS) analysis and frontier molecular orbital (HOMO-LUMO) analysis were integrated to understand the hydrogen bonding interaction more comprehensively. The simulation results are in good agreement with the experimental data. The results show that the analysis of physical and chemical properties of TF-PNP cocrystal and TF crystal by quantum chemistry method is reliable at molecular level. These results are helpful to provide guiding methods in the cocrystal development and theoretical study of tegafur.

Novel bioequivalent oral disintegrating tablet of aripiprazole prepared by direct compression technique with shortened disintegration time

Herein, we aimed to formulate a novel oral disintegrating tablet (ODT) of aripiprazole (ARP) capable of rapid disintegration using a direct compression technique. Different ODTs were fabricated with directly compressible excipients, and their disintegration time, wettability (water absorption ratio and wetting time), and mechanical properties (hardness and friability) were evaluated. The optimized ODT comprised F-Melt® type C, Prosolv® SMCC HD90, and Na croscarmellose (10 mg of ARP in a 130 mg tablet). The ODT with 3.1–5.2 kp hardness exhibited rapid disintegration (14.1–17.2 sec), along with appropriate mechanical strength (friability < 0.24%). In a bioequivalent study in Korean healthy subjects (randomized, single-dose, two-period crossover design, n = 37), the novel ODT offered the equivalent pharmacokinetic profile to that of a conventional immediate release tablet (Otsuka, Abilify®, Japan), despite different disintegration and dissolution profiles. The 90% confidence intervals of the geometric mean test to reference ratios considering the area-under-the-curve and maximum plasma drug concentrations were 1.0306–11051 and 0.9448–1.1063, respectively, satisfying FDA regulatory criteria for bioequivalence. The novel ART ODT was physicochemically stable under the accelerated storage condition (40 °C, RH75%) for 24 weeks. Therefore, the novel ARP-loaded ODT is expected to be an alternative to oral ARP therapy, providing improved patient adherence.

Shedding light on the ageing of extra virgin olive oil: Probing the impact of temperature with fluorescence spectroscopy and machine learning techniques

This work systematically investigates the oxidation of extra virgin olive oil (EVOO) under accelerated storage conditions with UV absorption and total fluorescence spectroscopy. With the large amount of data collected, it proposes a method to monitor the oil's quality based on machine learning (ML) applied to highly-aggregated data.EVOO is a high-quality vegetable oil that has earned worldwide reputation for its numerous health benefits and excellent taste. Despite its outstanding quality, EVOO degrades over time due to oxidation, which can affect both its health qualities and flavour. Therefore, it is highly relevant to quantify the effects of oxidation on EVOO and develop methods to assess it that can be easily implemented under field conditions, rather than in specialized analytical laboratories.The ML approach indicates that the two excitation wavelengths (480 nm) and (300 nm) exhibit the maximum relative change in fluorescence intensity during the ageing for the majority of the oils, thus identifying the wavelengths which are more informative for quality prediction. Also, the paper proposes a method for the prediction of olive oil quality using highly-aggregated data. Such a method is of interest because it paves the way to the realization of a low-cost, portable device for in-field quality control.The following study demonstrates that fluorescence spectroscopy has the capability to monitor the effect of oxidation and assess the quality of EVOO, even when the data are highly aggregated. It shows that complex laboratory equipment is not necessary to exploit fluorescence spectroscopy using the proposed method and that cost-effective solutions, which can be used in-field by non-scientists, could provide an easily-accessible assessment of the quality of EVOO.

Design, Optimization and In vitro Evaluation of Mesalazine 400 mg Delayed Release Tablet for Colon Specific Delivery

Ulcerative colitis is a chronic inflammatory disease, and patients would get benefit more if the drug is given directly to the colon. Mesalazine is intended to deliver to the colon for treating ulcerative colitis. Here, we aimed to design and optimize mesalazine 400 mg delayed release tablet for colon-specific delivery using a quality by design (QbD) approach. The tablet was first formulated as an optimized core tablet and then coated with Eudragit S 12.5 for ensuring colonic delivery. The experimental design for the core tablet was constructed using a 32 full factorial design, where the percentages of sodium starch glycolate (SSG) and polyvinylpyrrolidone (PVP K-30) were independent variables and the tablet hardness (kg/cm2) and cumulative percentage of drug release at pH 7.2 phosphate buffer after 1.5 hours were treated as responses. Responses obtained from the initial exploratory formulations were evaluated to develop an optimized formulation to have a hardness value of 7-8 kg/cm2 and the maximum amount of drug release at pH 7.2 buffer. The optimized formulation involved the use of SSG and PVP K-30 at 3.05% and 1.69%, respectively. Hardness and cumulative percent of drug release obtained for the optimized core tablet were 7.8 kg/cm2 and 91.76%, respectively. The compatibility of drug and excipients was studied utilizing XRD, FTIR and TGA. The optimized core tablet was then coated with Eudragit S 12.5 to deliver the drug selectively to the colon and further assessed for its in vitro dissolution. Dissolution studies indicated that coated tablets with a weight gain of 7.4% exhibited the maximum cumulative percent of drug release (91.19 ± 0.11%), with a zero-order drug release profile (R2 = 0.943). A stability study performed according to ICH Q1A (R2) guidelines at accelerated storage conditions identified that there was no significant change in drug content over the storage period, indicating the stability of the formulated tablet batches. Together, these data suggest that the mesalazine tablet developed through the QbD approach offers excellent physical properties and drug release profile and, therefore, could be recommended for commercial manufacturing. Dhaka Univ. J. Pharm. Sci. 22(2): 189-201, 2023 (December)

GC-IMS determination of volatile organic compounds as potential indicators of wheat germination rate

The objective of this research was to investigate the correlation between volatile organic compounds (VOCs) and the germination rate of stored wheat, as well as to identify the potential markers for predicting the germination rate. The findings of this study are expected to contribute to the advancement of a non-destructive and rapid method for evaluating the quality of wheat storage, thereby establishing a theoretical foundation for further research in this area. Gas chromatography-ion mobility spectrometry (GC-IMS) was utilized to analyze the VOCs of wheat samples subjected to accelerated storage condition at 40 °C, RH 65%, as well as natural storage condition at room temperature. A total of 68 and 79 VOCs were detected under accelerated and natural storage conditions, respectively. The germination rate of wheat was found to decreased significantly with prolonged storage time under both storage conditions. Principal component analysis (PCA) and hierarchical cluster analysis (HCA) were utilized to differentiate wheat samples stored for varying durations. Furthermore, correlation analysis revealed that 31 VOCs exhibited a significant correlation (p < 0.05) with the germination rate. Through multiple linear stepwise regression analysis, four VOCs—namely isoamyl butyrate, (Z)-3-nonen-1-ol, 1-propanol, and Propanal—were identified as potential markers. Subsequently, a prediction model was constructed using these markers. The results of this study demonstrate that these VOCs can serve as indicators for predicting the germination rate, thus facilitating the evaluation of the germination ability and quality of stored wheat. This research holds implications for enhancing the efficiency of wheat storage management and ensuring food security.

Stabilization of infant formulas against lipid oxidation: What are the key structural levers?

AbstractInfant follow‐on formulas (IFF) mimic human milk. This study aimed to identify the key structural levers that influence oxidative stability of IFF. Representative model IFF of marketed products in term of lipid composition were formulated with varying droplet size, lipid droplet core composition, and interfacial composition using different emulsifiers (soy lecithin or dairy phospholipids [DPL]). The oxidative stability of model IFF was assessed in accelerated storage conditions. No significant stabilization effect based on the lipid droplet core composition was observed. However, the nature of the interface, influenced by the emulsifier type, had an impact. Model IFF with DPL showed no loss of tocopherols and peroxide value was up to twice lower than those with soy lecithin after 20 days. This effect was particularly pronounced for the 0.4µm droplets. These results suggest that model IFF with DPL had a greater oxidative stability, likely due to the presence of sphingomyelin and the formation of a rigidified domain at the droplet surface. Model IFF with 0.4 µm droplets stabilized with soy lecithin, especially when added to the water phase, showed a tocopherols loss twice as high as that of IFF with DPL. These results indicate that oxidative stability of IFF is more influenced by the chemical environment rather than droplet size.Practical Application: Infant follow‐on formulas (IFF) aim to ensure an adequate nutritional intake to support the proper development and infant growth. Therefore, IFF must be stable against degradation phenomena such as lipid oxidation and have a composition and structure that are as biomimetic as possible to mature breast milk. This study provides key information for the development of IFF with a lipid composition and structure that are suitable for the infant nutritional needs and have an acceptable resistance to lipid oxidation. More generally, these results can be applied to all dispersed systems in the form of oil‐in‐water emulsions with a similar composition.

Synergistic impact of arbutin and kaempferol-7-O-α-l-rhamnopyranoside from Nephelium lappaceum L. on whitening efficacy and stability of cosmetic formulations

Four flavonoid glycosides, namely quercetin-3-O-rhamnoside (1), kaempferol-3-O-β-d-glucopyranosyl (2), kaempferol-7-O-α-l-rhamnopyranoside (3), and kaempferol-3-O-β-d-glucopyranosyl-7-O-α-l-rhamnopyranoside (4), from Nephelium lappaceum L. seeds were evaluated for their efficacy against melanin inhibition in B16F10 melanoma cells and tyrosinase inhibition. Among them, kaempferol-7-O-α-l-rhamnopyranoside (3) displayed the highest potency in both activities without any significant cytotoxicity. The combination of compound 3 and arbutin in specific proportions demonstrated a synergistic effect (CI < 1) in inhibiting melanin production in B16F10 cells and tyrosinase inhibition. Additionally, a cosmetic formulation containing compound 3 and arbutin as active ingredients exhibited favorable stability under accelerated storage conditions. Quantitative analysis indicated that compound 3 and arbutin levels in the formulation were above 90% after one month of storage. Determination of the formulation's shelf life using the Q10 method, estimating it to be around 5.2 months from the date of manufacture. The synergy between arbutin and kaempferol-7-O-α-l-rhamnopyranoside (3) extracted from N. lappaceum substantially enhances both the whitening effectiveness and the stability of cosmetic formulations.

Development and assessment of gastro retentive floating tablets of celiprolol using natural polymers

Gastro retentive floating tablets are a promising drug delivery system for improving the bioavailability and therapeutic efficacy of orally administered drugs, particularly those with a narrow absorption window in the gastrointestinal tract. In this study, we aimed to develop and evaluate gastro retentive floating tablets of Celiprolol using natural polymers. The tablets were formulated by incorporating a combination of natural polymers, including hydroxypropyl methylcellulose (HPMC) and sodium alginate, to achieve buoyancy and sustained drug release. Various formulation parameters, such as polymer concentration, drug-to-polymer ratio, and effervescent agents, were optimized to attain desired tablet characteristics. The prepared tablets were evaluated for their physical characteristics, floating behavior, drug release profile, and drug stability. The optimized formulation demonstrated excellent floating properties, with a floating lag time of less than 60 seconds and a floating duration of more than 12 hours. In vitro drug release studies revealed sustained release of Celiprolol from the tablets over a period of 12 hours. The drug release kinetics followed the Higuchi model, suggesting diffusion as the predominant mechanism. Stability studies indicated that the floating tablets maintained their physical and drug release characteristics over a period of six months under accelerated storage conditions. Overall, the developed gastro retentive floating tablets of Celiprolol using natural polymers showed promising characteristics in terms of floating behavior, sustained drug release, and stability. This formulation has the potential to improve the therapeutic outcomes of Celiprolol by enhancing its bioavailability and ensuring prolonged drug exposure in the gastrointestinal tract. Further in vivo studies are warranted to validate the efficacy and pharmacokinetic profile of these tablets for potential clinical applications in the treatment of hypertension and other cardiovascular condition.