Journal of Applied Pharmaceutical Research (JOAPR)
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Chitosan-based mucoadhesive patches for buccal delivery of olmesartan in hypertension treatment
Get PDFBackground: Delivering poorly soluble drugs like Olmesartan (OMS) effectively remains a key challenge due to low oral bioavailability and extensive first-pass metabolism. To address this, buccal patches incorporating chitosan were developed as an alternative route to enhance systemic absorption. Methodology: A series of buccal patch formulations (F1–F17) was prepared using combinations of chitosan, polyvinyl alcohol (PVA), HPMC K4M, and Eudragit RL via solvent casting. These patches were evaluated for uniformity in weight, thickness, pH, mechanical strength, folding endurance, and mucoadhesion. Structural and morphological assessments were carried out using X-ray diffraction and SEM. Ex vivo and in vivo studies explored drug release, permeation, pharmacokinetics, and mucosal safety. An HPLC method was employed for accurate quantification, and stability was assessed under both accelerated and ambient conditions. Results and Discussion: The optimised patch (F2) demonstrated consistent physical properties, high flexibility, and strong mucoadhesion. XRD patterns confirmed the amorphous dispersion of OMS in the polymer matrix, aiding solubility. Drug release was sustained over 12 hours, and permeation studies showed controlled transport across the buccal membrane. In vivo results revealed a substantial improvement in drug bioavailability via buccal delivery (83.2%) compared to oral administration (30.2%). Histological analysis indicated no signs of tissue irritation. Patches maintained integrity and potency throughout six months of storage. Conclusion: The findings support the buccal patch as a viable, non-invasive platform for enhancing OMS delivery, offering improved therapeutic efficiency and patient compliance
A novel mucoadhesive nanofabrication strategy for levofloxacin hemihydrate optimized via central composite design for Helicobacter pylori therapy
Get PDFBackground: Helicobacter pylori (H. pylori), a gram-negative bacterium that causes gastritis, peptic ulcers, and gastric cancer, infects more than half of the global population. The recommended levofloxacin-based nanotherapy can be deployed to overcome rapid gastric emptying of the drug, inadequate drug concentration at the site of action, and the protective mucosal layer. The research established a goal to design and enhance Levofloxacin Hemihydrate(LH) Mucoadhesive Nanoparticles (LMNP) for better drug retention on stomach mucosa and mucosal adhesion, site-specific prolonged drug delivery against H. pylori. Methodology: The LMNP nanoparticles were prepared through ionic gelation of chitosan (CT), carbopol 974P(CP), and N-Acetylcysteine (NAC) before optimizing them using Central Composite Design (CCD) within Response Surface Methodology. The study used FTIR, DSC, XRD, SEM, particle size, zeta potential, entrapment efficiency (EE%), in vitro cumulative drug release %, and mucoadhesive strength (MS%) tests for characterization. Results and Discussion: The optimized LMNP formulation had a particle size of 245.4 ± 1.254 nm, an EE% of 72 ± 2.246%, and Prolonged drug release over 6 hours with in vitro CDR of 99.98 ± 0.115%, which fits the gastric mucus turnover time. FTIR, DSC, and XRD confirmed the compatibility of drug excipients. SEM revealed uniform spherical particles, and MS% was 62 ± 2.315%. The size of the particles and their entrapment efficiency , mucoadhesive properties, and in vitro cumulative drug release were influenced by CT and CP, but NAC enhanced mucopenetration effects. The CCD model successfully established formulation behavior and confirmed synergistic interactions among the excipients. By enhancing matrix formation and swelling, the combined impact of CT and CP significantly influenced. Conclusion: The LMNP system developed by employing CCD designs and ionic gelation methodology demonstrated promising characteristics for gastric retention and prolonged drug release , which could enhance H. pylori clearance rates. The drug delivery platform presents a practical, biocompatible solution to address challenges in conventional therapy
Phytochemical characterization and investigation of bioactivities of Melochia corchorifolia L.
Get PDFBackground: Melochia corchorifolia L. (MC) is traditionally used to treat various ailments. This study investigated its phytochemical content and evaluated its antioxidant, analgesic, anti-inflammatory, and hypoglycemic potential. Methodology: Standard phytochemical screening was conducted, and advanced chemical analyses were performed using GC-MS and HPLC. In vitro antioxidant effects were investigated using various methods. The in vivo analgesic effect was evaluated using the writhing and paw-licking tests. The anti-inflammatory effect was studied using the ear edema & granuluma formation tests. Hypoglycemic effect was assessed using OGTT. Results and Discussion: The standard screening test detected carbohydrates, glycosides, alkaloids, flavonoids, saponins, tannins, steroids, and phytosterols. Advanced analyses using GC-MS identified 75 compounds, including 8 major constituents, and HPLC quantified 5 polyphenols: catechin hydrate, (-)-epicatechin, vanillic acid, rutin hydrate, and rosmarinic acid. Significant levels of flavonoids and phenolics were present in the extract, which demonstrated moderate antioxidant capability in the DPPH assay (IC50: 287.35 µg/mL). A significant reduction in pain was observed with the acetic acid (p<0.01) and formalin (p<0.01) methods. The extract showed significant anti-inflammatory activity in the xylene- and croton oil-induced ear edema tests (p< 0.001 and p < 0.01), moderately suppressed granuloma formation, and significantly reduced blood glucose levels in the oral glucose tolerance test (p < 0.001). Conclusion: M. corchorifolia contains multiple bioactive compounds with promising antioxidant, analgesic, anti-inflammatory, and hypoglycemic properties, supporting its traditional medicinal use and suggesting its potential for further therapeutic research
Ethnobotanical survey of medicinal plants for bone fracture treatment in Lingmoo, Sikkim
Get PDFBackground: This study documents the use of herbal plants by traditional healers in Lingmoo, Namchi district, Sikkim, to treat bone fractures. Methodology: The methodology used were survey-based, pre-structured questionnaire, field investigation and face to face interaction with one traditional healer. We have recorded about 29 ethno-medicinal plants naturally available in the selected area. Results: According to the survey results, a total of 29 numbers of ethnomedicinal plant species belonging to 23 different families (Rosaceae topped the list) were identified and summarized in Table 1. The study revealed that herbs (48%) are mainly used, followed by trees (24%), climbers (17%), and shrubs (11%). In case of frequency of use, these plants were highly cited during the interview: rivularis, Kaempferia rotunda, Viscum articulatum, Urtica dioica, Curcuma longa, Lepidium sativum, Beaumontia grandiflora, Bergenia ciliate, and Laportea bulbifera. The parts used were roots, stem barks, whole plants, and seeds. The most commonly used preparation was paste. According to gender-wise comparison, males (60%), females (25%), and children (15%) were getting the treatment. Out of 29 plant species, 12 species are abundant and, 1 is in threatened condition; only 3 species are cultivated in present days. Conclusion: Documentation of local plants used by a specific traditional healer will benefit the sustainable use of indigenous medicinal plant practices. It will also provide preliminary information for future biological resource management and research development, which will eventually help in the conservation of ethnomedicinal plants and the advancement of such ideas
Exploring the therapeutic potential of Eleusine indica plant: promising antioxidant and analgesic activity with lack of antimicrobial and thrombolytic activity
Get PDFBackground: Eleusine indica is used as a traditional medicine in Bangladesh. It is significantly valued for its wound-healing properties and is often used as an anthelmintic and pain reliever in rural areas. Objective: This study examines the pharmacological effects of Eleusine indica methanolic extracts, highlighting antioxidant, antimicrobial, thrombolytic, and analgesic properties in animal models. Also, contribute to future research directions. Methods: The antioxidant properties were determined using the DPPH free radical scavenging assay, with ascorbic acid as the positive control, and the inhibition percentage was calculated. Antimicrobial activity was determined using the disc diffusion method. The thrombolytic Potential was determined through in vitro clot lysis assays. However, the % of clot lysis was used to gauge the thrombolytic effects. For assessing analgesic activity, Swiss albino mice were utilized; analgesic efficacy was evaluated by calculating the percentage inhibition against abdominal writhing. Results: The free radical scavenging assay demonstrated with an IC50 of 43.67 μg/ml, comparable to ascorbic acid's IC50 of 36.22 μg/ml. However, the methanolic extract showed no antimicrobial activity. In thrombolytic assays, the extract induced 26.79% clot lysis. With a 55.57% reduction in writhing, the extract group (500 mg/kg) exhibited significant analgesic activity, approaching the standard group's 73% inhibition. Conclusion: The Outcome of the study shows Eleusine indica has potential antioxidant and analgesic activity, with a lack of antimicrobial and thrombolytic properties. The results support the application of traditional medicine. highlighting the importance of antioxidant and analgesic activity, in future investigations aimed at isolating and identifying the specific compounds driving its pharmacological activities
A comprehensive review of peptic ulcer disease: epidemiology, experimental models, and mechanistic insights
Get PDFBackground: Peptic ulcer disease (PUD) is one of the most common gastrointestinal disorders, resulting from an imbalance between aggressive and protective factors, leading to mucosal erosion. Various factors influence its pathogenesis, including Helicobacter pylori infection, NSAID use, and oxidative stress. Objective: We review PUD epidemiology, varying experimental models, and mechanistic insights into PUD and promising therapeutics. Methodology: We systematically reviewed previous literature on PUD, including epidemiological trends, commonly used in vivo, and molecular mechanisms. Results and discussion: The global prevalence of peptic ulcer disease (PUD) follows an epidemiological pattern influenced by geography, lifestyle, and genetic factors. Experimental models using ethanol, NSAIDs, or Helicobacter pylori induction provide valuable insights into disease progression and pathophysiology. Emerging trends: Recent research in peptic ulcer disease focuses on molecular mechanisms, gut microbiome interactions, personalized therapies, and novel pharmacological agents. Molecular studies explore genetic and epigenetic factors influencing ulcer formation, while microbiome research examines the role of gut bacteria beyond H. pylori. Personalized treatment approaches use genetic profiling and biomarkers to enhance efficacy and reduce toxicity. Additionally, emerging pharmacological agents aim to improve acid suppression, promote mucosal healing, and develop more effective H. pylori eradication strategies. Conclusion: A deeper understanding of PUD pathophysiology through epidemiological studies and experimental models can aid in developing novel, targeted therapies. Future research should focus on alternative treatments, including phytochemicals and probiotics, to enhance ulcer prevention and management
Chitosan-coated CMC and carbopol hydrogel beads for controlled release of metformin in diabetes management
Get PDFBackground: Current research aims to fabricate carboxymethyl cellulose sodium (CMC-Na) and carbopol hydrogel beads. Gleichzeitig, beads were coated with chitosan to enhance the controlled release of the drug Metformin HCl (MET), which serves as a model drug for diabetes mellitus (DM). Methodology: The MET beads were synthesized through the ionotropic gelation process. The foundation of ionotropic gelation is a polyelectrolyte’s capacity to cross-link to create hydrogels when counterions are present. The negatively charged carboxylate groups (-COO⁻) on CMC-Na form electrostatic interactions with the positively charged aluminium ions (Al³⁺) from AlCl3. The quality-by-design approach was employed to optimize process factors in preparing hydrogel beads. A comprehensive evaluation of the beads covered various aspects such as particle size, scanning electron microscopy, percentage yield, Fourier transform infrared spectroscopy, X-ray diffraction, entrapment efficiency (EE), and in vitro drug release. Results and Discussion: The beads were spherical, with an average particle diameter of 153.6 to 231.5 μm. The entrapment efficiency percentage range is 94.4% and 97.83% for MET-loaded and chitosan-coated MET-loaded beads, respectively. Therefore, in-vitro drug release of the optimized MET-loaded beads is 55.5 %, and chitosan-coated MET-loaded beads are approximately 48.8% achieved in 10 hours. Conclusion: Chitosan-coated CMC-Na and carbopol hydrogel beads showed good MET encapsulation and sustained release, improving structural integrity and drug release. The ionotropic gelation process created stable, homogeneous beads, making this delivery method viable for oral sustained-release MET formulations
Development and evaluation of an amorphous solid dispersion-based probucol immediate-release tablet
Get PDFBackground: In its crystalline form, probucol has an extremely low bioavailability and is a poor water-soluble drug. The main aim of this study was to enhance the solubility and dissolution rate of probucol by using a solvent evaporation method to develop a solid dispersion that contains polyvinyl pyrrolidone K30 (PVP-K30) and polyethylene glycol 6000 (PEG 6000). Methodology: The solvent evaporation method is considered superior to other techniques for preparing solid dispersions due to its ability to achieve uniform drug distribution at the molecular level. This method ensures homogeneity by dissolving the drug and carrier in a common solvent, reducing the risk of drug recrystallization and enhancing solubility and bioavailability. Result: The drug-to-carrier ratio is the determining factor for dissolution enhancement. The FTIR spectra do not suggest any chemical interaction between PVP-K30 or PEG 6000. The immediate release profiles of both formulations were favourable, with F3 releasing approximately 95.31% of the drug and F6 releasing around 86.77% within 2 hours. This indicates a rapid drug dissolution, which is beneficial for achieving a fast onset of action and enhancing bioavailability. Conclusion: The solid dispersion formulations F3 & F6 successfully transformed crystalline probucol to an amorphous state, enhancing solubility & dissolving rates appropriate for immediate-release tablets
Heterocyclic scaffolds in antibiofilm strategies against drug-resistant pathogens: a comprehensive review
Get PDFBackground: Antimicrobial resistance (AMR) is a primary global health concern, exacerbated by the ability of drug-resistant pathogens to form biofilms. These biofilms, which harbor microbial communities embedded in an extracellular polymeric matrix (EPS), enhance antibiotic resistance and immune responses, leading to persistent infections. Heterocyclic compounds have shown significant potential in combating biofilm-associated infections due to their structural diversity and mechanisms of action. Methodology: This review systematically examines the antibiofilm potential of various heterocyclic scaffolds, including imidazoles, pyrazoles, indoles, quinolines, coumarins, and select six-membered heterocycles (pyridine, morpholine, piperazine). Studies were analyzed based on their mechanisms of action, structure-activity relationships (SAR), and synergy with conventional antibiotics. Result and Discussion: Imidazole derivatives disrupted biofilm integrity and enhanced antibiotic susceptibility in Pseudomonas aeruginosa and Staphylococcus aureus, with IC50 values ranging from 0.53 to 9.5 µM. Pyrazole-based compounds inhibited Staphylococcus epidermidis biofilms, with IC50 values ranging from 3.1 to 15.6 µg/mL. Indole derivatives, particularly pyrroloindoline triazole amides, inhibited MRSA biofilms with IC50 values as low as 2.8 µM by targeting quorum sensing and curli production. Quinoline compounds demonstrated greater than 90% inhibition of E. coli and P. aeruginosa biofilms and showed synergistic effects with antibiotics. Conclusion: Heterocyclic compounds exhibit promising antibiofilm activity, presenting a viable approach to overcoming AMR. These compounds not only disrupt biofilm formation but also enhance the efficacy of conventional antibiotics through synergistic interactions. Such synergy potentiates the antimicrobial effect by improving antibiotic penetration or disrupting resistance pathways. Future research should focus on optimizing pharmacokinetics and exploring these synergistic combinations to improve clinical applicability
Formulation and evaluation of ethosomal gel containing Nyctanthes arbor-tristis leaf extract using design of experiments for enhanced topical delivery
Get PDFBackground: Nyctanthes arbor-tristis (L.), generally known as Night Jasmine, is a medicinal plant renowned for its antimicrobial and antioxidant activities. Despite its traditional therapeutic use, there is limited scientific research on its detailed botanical characterization, phytochemical composition, and incorporation into advanced pharmaceutical formulations. This study aims to fill this gap by investigating the botanical and phytochemical profiles of N. arbor-tristis leaves and by developing optimized ethosomal gel formulations for enhanced topical drug delivery. Methodology: Comprehensive phytochemical screening revealed the existence of steroids, alkaloids, flavonoids, and tannins. Quality control parameters such as moisture content and ash values were evaluated. Ethosomal gels were prepared with phospholipids, cholesterol, and ethanol, and formulation optimization was performed using a Design of Experiments (DoE) approach. The developed formulations were systematically evaluated for particle size, polydispersity index, zeta potential, entrapment efficiency, and in vitro drug release profiles. Result and Discussion: Optimized formulations (EG-NAT-12 and EG-NAT-11) exhibited favorable nanoscale particle sizes (130.0 nm and 132.5 nm), low polydispersity indices (0.258 ± 0.027 and 0.274 ± 0.029), high negative zeta potentials (−23.5 mV to −24.0 mV), and high entrapment efficiencies (up to 89.8%). EG-NAT-12 demonstrated sustained drug release, with 84.0% released over 6 hrs. Stability testing confirmed the physical and chemical stability of the formulations over 45 days at both refrigerated and room temperatures. Conclusion: This study demonstrates the potential of Nyctanthes arbor-tristis ethosomal gels as effective topical drug delivery systems, integrating traditional herbal benefits with modern nanotechnology to enhance their efficacy