Journal of Applied Pharmaceutical Research (JOAPR)
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Development and in vitro evaluation of acelofenac mouth dissolving films for reduced analgesic activity
Get PDFBackground: The design of the current research work was to formulate mouth-dissolving films (MDFs) of aceclofenac (ACF) to improve patient compliance and convenience for older and younger patients, ultimately leading to improved therapeutic outcomes. Method: Evaluations were conducted on film formers such as HPMC and MC and film modifiers such as PEG and starch acting as solubilizing agents. Results: The physicomechanical qualities, in vitro disintegration time, and in vitro dissolving characteristics of the produced MDFs were assessed. Good mechanical qualities, including as tensile strength, folding durability, and percentage elongation, were demonstrated by every created MDF. FTIR, SEM, and X-RD analyses were used to assess MDFs. In contrast to other formulations, MDFs containing F8 provided superior dissolving properties. Conclusion: When pitted against other mixtures, the MDFs with sodium alginate (5%), methylcellulose (5%), and hydroxypropyl methylcellulose (HPMC)(5%) showed superior dissolving capabilities. In contrast to other mixtures, the F8 mixture, including HPMC, sodium alginate, and methylcellulose, demonstrated a complete and accelerated dissolution within 50 seconds. The mechanism behind this release is diffusion, as indicated by the release kinetics data
Doxorubicin-induced cardiotoxicity: An update on the molecular mechanism, biomarkers and management
Get PDFBackground: Doxorubicin (DOX) is a widely used chemotherapeutic agent that is effective against various solid tumors and hematologic malignancies. However, its clinical application is severely limited by dose-dependent cardiotoxicity, which affects nearly 26% of patients. Objective: This review focuses on recent insights into the molecular mechanisms of DOX-induced cardiotoxicity, particularly highlighting the roles of oxidative stress and mitochondrial dysfunction. Methods: We have reviewed and retrieved the relevant information by probing the main keywords in online databases (PubMed, Scopus, Science Direct and Web of Science, etc.). Screening of relevant literature was done to pick suitable content based on the pharmacological profile of DOX. Key biomarkers such as troponins, brain natriuretic peptides (BNP), and atrial natriuretic peptides (ANP) are crucial for early detection of cardiac injury. The overproduction of reactive oxygen species (ROS) and reactive nitrogen species (RNS), mediated by enzymes like NADPH oxidase and mitochondrial cytochrome c, is central in triggering apoptosis and cardiomyocyte damage. Furthermore, DOX’s impact extends to other organs, notably the liver and kidneys, contributing to systemic toxicity. Conclusion: This review synthesizes current strategies to mitigate DOX-induced cardiotoxicity, including applying antioxidants, liposomal DOX formulations, and emerging nanocarrier technologies designed to enhance therapeutic selectivity. Looking ahead, integrating personalized medicine approaches and developing innovative therapeutic interventions hold promise for balancing DOX's antitumor efficacy with a reduced risk of cardiotoxicity. By addressing critical gaps in our understanding, this review highlights the need for integrative approaches combining biomarker discovery and targeted therapies to optimize patient outcomes and guide future research directions
Development and evaluation of extended-release vildagliptin tablets using quality by design
Get PDFBackground: Extended-release dosage forms are designed to enhance patient compliance and decrease dosing frequency. However, commercially available extended-release tablets are made with synthetic or semisynthetic controlled-release polymer, which causes a ghost pill effect. The ghost pill effect is minimized by using natural polymers which are biodegradable. Aim: This study aimed to create extended-release vildagliptin tablets using natural polymer by employing the quality by Design. Method: The study involved preparing granules of vildagliptin by direct compression using co-processed polymer and other excipients and compressing them into tablets. Results & Discussion: The different micromeritic characteristics of granules were satisfactory for compressing them into tablets. The FTIR, DSC, and XRD analysis indicates no interaction between the drug and the other excipients. The drug release shows that the marketed formulation releases 97% of the drug in 8 hrs., Whereas the developed formulation extends the drug release >= 95% throughout 12hrs. Drug release kinetic study results reveal that the optimized batch obeys first-order kinetics with the Higuchi model. In vivo studies showed steady plasma levels over an extended period, achieving the objective of the current study. The stability study carried out as per the ICH guideline exhibited robustness of the formulation, with the drug content found between 96 % to 99 % at 30°C & 75 %RH and 40°C & 75 %RH. Conclusion: The extended-release formulation of vildagliptin could be successfully formulated using a combination of natural and semisynthetic polymers. This combination could prove to be effective, safe, and well tolerated, enhancing patient adherence and lowering overdose risks, thereby reducing overall diabetic treatment costs
Isolation, purification, and characterization of bioactive peptide from Chenopodium quinoa seeds: therapeutic and functional insights
Get PDFBackground: Chenopodium quinoa is a nutrient-dense pseudocereal packed with proteins, vital amino acids, and bioactive substances that may have medicinal uses. These include antioxidant, anti-inflammatory, anti-cancer, and antibacterial properties. Notably, quinoa proteins and peptides show multifunctional bioactivities such as immunological regulation, cancer cell death, and microbial suppression. This study aimed to separate, purify, and describe the bioactive proteins found in quinoa seeds, emphasizing their potential applications as medicines. Methodology: Quinoa seeds underwent protein extraction, defatting, and de-saponification. Ion exchange chromatography, dialysis, and ammonium sulfate precipitation were used to purify the seeds. The Lowry technique was used to quantify the proteins. Functional tests assessed the seeds' antibacterial, antifungal, protease, and anticancer properties, and peptide identification was carried out using LC-MS/MS. Results: The protein content decreased during purification steps, indicating effective removal of impurities. Protein fractions exhibited significant antibacterial and antifungal activities. Protease activity varied among fractions, with the pH 2 fraction showing the highest activity. Crude extract and pH 2-treated fractions demonstrated significant anticancer activity against A549 and Hela cell lines. pH 2 fraction exhibits the highest protease activity of 2.451 units/ml, indicating enhanced enzymatic capability under acidic conditions. Peptides identified from the pH 2 fraction showed potential therapeutic properties. Conclusion: The antibacterial, antifungal, proteolytic, and anticancer properties of quinoa-derived peptides and proteins demonstrate their potential for use in medicine. Clinical validation and the creation of functional foods or nutraceuticals based on quinoa should be the main objectives of future research
Formulation and standardization of lohasava: an ayurvedic aasava formulation Man
Get PDFBackground: Plant solutions or decoctions are fermented with added sugar to create alcoholic remedies like arishta and aasava. Standardizing ayurvedic formulations is essential to assessing the quality of medicine. Objective: Standardisation of Lohasava, which contains iron as a metal and is used as hematinic, has been carried out in the current study. Methods: The standard ayurvedic procedure was used to prepare the aasava formulation. Modern scientific control processes have standardized the formulation for the final products. Organoleptic analysis, phytochemical assessment, and physicochemical characteristics such as pH, specific gravity, viscosity, acid values, total solid content, alcohol content, heavy metal content, and stability studies were used to standardize asava. Additionally, formulations were examined for the presence of pesticides. Using UV-visible spectrophotometric analysis, the iron content was determined. Animal studies were carried out to evaluate pharmacological activity. Results: Physical and chemical parameters were found within limits. The alcohol content of formulations was within limits and indicated good fermentation. Conclusion: The study's findings have revealed good formulation quality and provide a standard for aasava and ayurvedic formulations
Cinnamomum impressinervium meisn.: antioxidant and antimicrobial activities
Get PDFBackground: The Cinnamomum impressinervium (CI) Meisn. Tree, which belongs to the Lauraceae family and is endemic to India, is also called Assameses or Tejiya. Numerous pharmacological properties of this plant, including anti-tumor, anti-inflammatory, and antioxidant properties, have been demonstrated. Materials and method: This study examines the phytochemical profile of the leaf using qualitative and quantitative methods. Following the phytochemical analysis of the leaf, the antioxidant efficacy for scavenging free radicals (ABTS and DPPH) was measured. Using the agar well diffusion method, the antibacterial potential of the crude extract and its fractions (aqueous, methanolic, n-hexane, and chloroform) was investigated against six gram-negative, three gram-positive, and one fungal strain. Result and discussion: Antioxidant activities of various extracts viz: aqueous, hexane, chloroform, and ethanol were prepared and subjected to antioxidant and antimicrobial activities. Through qualitative analysis, several alkaloids, steroids, and flavones were identified. In the DPPH and ABTS assays, the aqueous extract had the most potent antioxidant activity, with IC50 values of 123.83±0.42 and 57.86±0.85 μg/mL, respectively. DNA nicking assay is a qualitative analysis that shows DNA protection from free radicals. All the extracts towards B. atropheous showed best inhibition activity but a maximum zone of inhibition was shown by aqueous extracts measuring 40 mm. Aqueous and methanolic extracts are completely inactive towards S. typhi. Conclusion: This study revealed the antioxidant and antimicrobial efficacy of various extracts of Cinnamomum impressinervium Meisn. Leaves In this paper, the antibacterial activity of leaf extracts from Cinnamomum impressinervium Meisn. were studied. The evaluated extracts showed varied levels of inhibitory zones against every tested bacterium
A single centre, real world experience of T-DM1 in the treatment of HER2-positive metastatic breast cancer patients in India
Get PDFBackground: HER2 (Human Epidermal Growth Receptor 2) positive breast cancer is an aggressive subtype. Treatment for patients with HER2-positive breast cancer has advanced significantly over time with the introduction of targeted therapies like trastuzumab, pertuzumab, lapatinib, trastuzumab emtansine, trastuzumab, deruxtecan, and tucatinib. In a lower-middle-income nation, accessibility is still problematic for any newer therapy. This study aimed to describe the safety and practical effectiveness of the first T-DM1 biosimilar in India for treating patients with HER2-positive mBC. Methodology: This is a retrospective, observational, single-center study of patients with HER2-positive metastatic breast cancer treated with T-DM1 biosimilar. The study involved 16 mBC patients. The primary goal was to assess T-DM1's effectiveness regarding PFS and ORR, with safety and OS as the secondary goals. Results: The ORR was observed to be 81.3%. One (6.29%) of the patients achieved CR, while 3 patients (18.8%) are on stable disease, and 12 patients (75 %) achieved PR. The major adverse events reported among study patients were thrombocytopenia (31.25%) and anemia (31.25%), followed by neutropenia, hyperglycemia, and fatigue in 12.5 % of cases. Grade 3 thrombocytopenia was seen in 2 patients, and grade 3-4 fatigue was observed in 1 patient. Median PFS was nearly six months, and OS data is available for only 25% of patients; the rest continue the therapy. Conclusion: This retrospective observational study offers significant information about the safety and efficacy of T-DM1 biosimilar in treating HER2 positive mBC
Formulation, development, and characterization of loratadine emulgel
Get PDFBackground: This study was to develop loratadine (LTD) emulgels to treat localized skin allergy. Method: Initially oil-in-water emulsion was prepared by 3 different types of surfactants & finally gelling agent carbopol 940 was incorporated into emulsion to produce emulgel (i.e., standard conventional method). Results: The developed formulations were characterized using various parameters including particle size (PS), zeta potential (ZP), polydispersity index (PDI), entrapment efficacy (EE), pH, extrusion efficacy, physical stability, in-vitro drug release studies, and scanning electron microscopy (SEM). PS, EE, PDI, ZP and In-vitro studies ranges between 186.25 ± 6.42 mm (LE-F4) to 395.24 ± 8.64 mm (LE-F1), 62.38 ± 0.36 % (LE-F2) to 76.48 ± 0.69 % (LE-F4), 0.276 ± 0.02 (LE-F4) to 0.652 ± 0.02 (LE-F1), 16.45 ± 2.13 mV (LE-F1) to 29.46 ± 2.78 mV (LE-F3) and 21.90 ± 0.3 % (LE-F1) to 68.30±0.9 % (LE-F4) respectively. Conclusion: Based on all physicochemical properties, LE-F4 formulation was considered to be optimized with minimum PS (186.25±6.42 nm), PDI (0.276±0.02), satisfactory positive surface charge (23.15 ± 1.89 mV) and maximum EE (76.48±0.69 %). FTIR studies were confirmed that there is no physical interaction between drug and excipients and SEM studies revealed that vesicle size was spherical with smooth texture. A significantly greater rate of drug release (i.e., 68.30 ± 0.90%) was seen in the LTD emulgels that were made with cationic surfactant (i.e., LE-F4) and found to be good spreadability and extrudability
Investigating the role of sesamol in promoting the healing of diabetic wounds by analyzing molecular expression patterns in human diabetic dermal fibroblasts.
Get PDFBackground: Sesamol (3,4-methylenedioxyphenol) is one of the plant compounds tested in vivo for diabetic wound healing, normal wound healing, and dexamethasone-induced delayed wound healing. Elucidation of mechanisms underlying the wound healing effect of sesamol through modulation of various molecular and cellular pathways is the crux of this paper. Objectives: The objective of the current work was to uncover the mechanism of sesamol underlying the treatment of diabetic wounds using gene expression analysis. Methods: The cytotoxicity assay was performed using an SRB colorimetric assay, from which two doses were selected for further studies. The expression of various molecular markers was performed using RT-PCR. Results: An SRB assay was carried out to identify the safe concentration of molecules in HDDF cell lines. Two doses that showed more than 80 % viability were selected and used for gene expression analysis. It was observed that sesamol enhanced the expression of VEGF, TGFβ, AKT, JNK, ERK, and TIMP3 significantly (P≤0.001, P≤0.05, P≤0.001, P≤0.0001) when compared to control and significantly (P≤0.0001) downregulated the expression of MMP2, MMP-9 when compared to control, which promote wound healing in diabetes. The migration studies also showed a significant increase when compared to the control. Conclusion: Sesamol (SM) is a promising molecule that can accelerate wound healing in diabetes by modulating different markers involved in the process
Evaluation of the hepatoprotective and nephroprotective properties of bael fruit extract against carbon tetrachloride-induced toxicity in rats
Get PDFBackground: Bael is well-known for its antibacterial properties. Aqueous fruit extracts have also been shown to have hepatoprotective properties; the nephroprotective and hepatoprotective properties of Ethanolic extracts have not yet been tested. Objective: To evaluate the hepatoprotective and nephroprotective activities of Bael against CCl4-induced toxicity in rats. Methods: Two dosages of Bael's Ethanolic extract (100 and 200 mg/kg/day) were compared with 100 mg/kg of silymarin. Histopathologic alterations of the liver and kidney, as well as biochemical blood parameters such as bilirubin, urea, uric acid, total protein and creatinine, alkaline phosphatase (ALP), alanine aminotransferase (ALT), were examined and assessed. Results: Bael was more successful in lowering high levels of urea, creatinine, ALT, AST, and ALP when he used a 200 mg/kg/day methanol extract. According to the histopathologic assessment, Bael lessened the CCl4-induced hepatic and renal necrosis. The more significant dose resulted in reductions in AST, ALT, GGT, ALP, and bilirubin of 45,25, 52,36, and 16%, respectively. Ethanolic extract 200 mg/kg/day also shows a reduction in elevated levels of Creatinine, Urea, Uric Acid, and Total Protein by 57%, 52%, 34%, and 9%, respectively. Conclusion: There were established hepatoprotective and nephroprotective effects of the Bael fruit methanol extract, with 200 mg/kg/day being the most beneficial dose. This provides scientific proof that medicinal herbs like Bael can be used to treat renal and liver diseases