Innovare Academic Sciences: E-Journals
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CHITOSAN-ROSE ESSENTIAL OIL FILMS: EVALUATION OF PHYSICAL INTEGRITY AND BIOPROTECTIVE ACTIVITIES
No full textObjective: To develop and characterize chitosan-based films enriched with rose essential oil as a natural, bioactive wound dressing.
Methods: Films were prepared using chitosan as the matrix polymer with rose essential oil incorporated at 0.5%, 1%, and 2% (w/w) concentrations. Physicochemical properties, antioxidant capacity, and antimicrobial activity were evaluated to assess their potential for wound healing applications.
Results: The films exhibited uniform thickness (0.15–0.22 mm) and weight (0.28–0.38 g) with skin-compatible pH (5.8–6.2). Swelling capacity wasdecreasedwithincreasingroseoil concentration (0.5%: ~250%, 1%: ~188%, 2%: ~120%), indicating controlled fluid uptake. Antioxidant activity rose in a concentration-dependent manner (0.5%: 35% ±2, 1%: 48% ±3, 2%: 62% ±4 DPPH inhibition). Antimicrobial tests showed increased inhibition zones versus control for S. aureus (12–18 mm vs 8 mm), E. coli (10–16 mm vs 7 mm), and C. albicans (8–14 mm vs 6 mm). These findings support enhanced bioactivity with higher rose oil loading.Conclusion: Chitosan films enriched with rose essential oil demonstrated favorable physicochemical, antioxidant, and antimicrobial properties, supporting their potential as effective natural wound dressings and bioactive delivery systems
THE COVID-19 CATALYST: A CRITICAL REVIEW OF ACCELERATED DRUG REPURPOSING STRATEGIES, LESSONS LEARNED, AND FUTURE DIRECTIONS
No full textObjective: To examine the significant effects of the COVID-19 pandemic on medication repurposing as a swift alternative to conventional drug development, highlighting algorithmic, omics-based, and clinical translation methodologies.
Methods: The COVID-19 pandemic is discussed starting with core concepts, encompassing definitions, classification systems, regulatory perspectives, and notable historical developments. For the reverse matching of drugs to illness profiles, we looked at both advanced computational tools and omics-based methods. The paper discussed flexible clinical trial approaches and how the rules were altered during the epidemic.
Results: Drug-candidate identification was shortened from years to months thanks to AI-assisted virtual screening, which enabled the rapid examination of thousands of approved compounds. About forty promising repurposed medications started clinical trials during the first year of the pandemic. Reliable efficacy results were rapidly produced by adaptive, data-driven trials, such as RECOVERY and ACTT. Successful medications like remdesivir, dexamethasone, and baricitinib showed definite benefits in recovery and mortality despite failures like hydroxychloroquine and lopinavir/ritonavir.Toxicity prediction and target matching were further enhanced by integrated chemical and biological databases, enabling quicker and more precise go/no-go determinations.
Conclusion: AI techniques, omics data, and adaptive clinisupervision, significantly reducing drug-development timescales from years to months without compromising regulatory oversight, as demonstrated by the COVID-19 pandemic. In addition to addressing obstacles such as off-target effects, regulatory limitations, intellectual property concerns, and limited model generalizability, the study emphasizes that future advancements will depend on the increased use of real-world evidence, precision-medicine-based repurposing, and open research collaboration
POLOXAMER-188 BASED CURCUMIN NANOEMULSION: FORMULATION, CHARACTERIZATION, AND STABILITY FOR ENTRAPMENT EFFICIENCY
No full textObjective: This study aimed to develop and characterize a curcumin-loaded nanoemulsion formulation to improve curcumin\u27s solubility and bioavailability using poloxamer 188, dimethyl sulfoxide (DMSO), tween-80, and polyethylene glycol 400 (PEG-400) as excipients.
Methods: Ten curcumin-loaded nanoemulsion formulations were optimized based on excipient combinations. These formulations were subjected to freeze-thaw cycles, particle size analysis, polydispersity index (PDI), zeta potential, differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), transmission electron microscopy (TEM), high-performance liquid chromatography (HPLC), and entrapment efficiency analysis to evaluate stability, solubility, and curcumin encapsulation efficiency.
Results: The study identified the optimal formulations (F5 to F8) based on their superior physical stability, as evidenced by minimal changes in viscosity and pH during freeze-thaw cycles. The entrapment efficiency of curcumin in these formulations ranged from 87.55% to 77.98%, indicating effective encapsulation. Characterization techniques, including DSC, HPLC, and FTIR, confirmed the stable incorporation of curcumin into the nanoemulsion with only minor structural modifications. The best formulation was demonstrated by Formula 5 with an average particle size of 195.3 nm, PDI of 0.36, and zeta potential of-16.2 mV. This formula showed uniform particle distribution and moderate colloidal stability among the other formulas. The TEM image showed spherical nanoparticles with smooth surfaces and consistent size distribution. Additionally, HPLC analysis of pure curcumin and nanoemulsion showed similar chromatographic profiles, confirming the stability and preservation of curcumin during the formulation process.
Conclusion: The optimized curcumin-loaded nanoemulsion demonstrated enhanced solubility and stability, with entrapment efficiency (EE) values ranging from 87.55% to 77.98%, indicating effective encapsulation of curcumin within the nanoemulsion system
MIXTURE DESIGN-BASED OPTIMIZATION OF DOLUTEGRAVIR SMEDDS USING JMP® SOFTWARE: BRIDGING PREFORMULATION TO PRODUCT DEVELOPMENT
No full textObjective: To address this challenge, the current research undertaken optimize the formulation of Self-microemulsifying drug delivery systems (SMEDDS)by applying structured Quality by Design (QbD) methodology.
Methods: Initial formulation development was guided by preformulation studies and pseudo-ternary phase diagram construction, as detailed in Part 1.An Extreme vertices mixture design in JMP® software was employed for systematic optimization. Ten SMEDDS formulations were prepared and assessed for key quality attributes: drug content, emulsification time, droplet size, and transmittance.
Results: The Optimized formulation included Capmul mcm c8 (0.183), Kolliphor EL (0.603), and Propylene Glycol (0.214). It showed rapid emulsification (45.66 seconds), high drug content (101.76%), fine droplet size (40.72 nm), and excellent clarity (99.22% transmittance). It also exhibited good thermodynamic stability, efficient self-emulsification (Grade A), and strong dilution tolerance. Liquid SMEDDS was made into a solid dosage form by adsorption onto Aerosil 200. The obtained S-SMEDDS exhibit acceptable flow properties, reflected by an angle of repose of 34.18°, Carr’s index of 17.87%, and a Haunser’s ratio of 1.21. It demonstrated high drug content uniformity (99.53%) and only a minimal increase in droplet size (46.2 nm), along with a zeta potential of –9.35 mV, confirming its physical stability.
Conclusion: Drug release studies showed enhanced drug release of (~100% within 60 minutes) from both liquid and S-SMEDDS indicating improved dissolution and potential bioavailability. The study supports S-SMEDDS as an effective delivery platform for poorly soluble drugs like DTG
TARGETING HUMAN FATTY ACID SYNTHASE IN CANCER THERAPY: STRUCTURAL INSIGHTS AND SAR OF DOMAIN SPECIFIC INHIBITOR
No full textFatty acid synthase is a key enzyme in humans that drives the biosynthesis of lipids essential for energy storage and cell membrane formation. Upregulation of FAS is significantly seen in cancer cells due to increased demands of lipids and cell proliferation. Cancer cells rely heavily on fatty acid synthesis to sustain their growth and maintain their malignant characteristics. Over the past two decades, FAS has gained considerable attention as a potential target for cancer therapy, as inhibiting this enzyme could disrupt lipid biosynthesis and impair cancer cell viability. Among the various inhibitors developed so far, TVB-2640 is the only one that has advanced into clinical trials. Here we discuss in detail about the structure and function of various domains of human fatty acid synthase enzyme with its inhibitors. In this review detailed of inhibitors for each domain are discussed. Review highlights how specific modifications to the inhibitor structure can enhance their binding affinity and selectivity towards each domain of FAS. By focusing on the Structural Activity Relationship, we aim to offer insights into the rational design of novel inhibitors that can effectively target FAS in cancer cells, thereby providing new avenues for cancer therapy
FORMULATION AND DEVELOPMENT OF GREEN-SYNTHESIZED ADAPALENE-CONJUGATED SILVER NANOPARTICLES INCORPORATED INTO ALOE VERA GEL FOR TOPICAL MANAGEMENT OF ACNE VULGARIS IN WOMEN
No full textObjective: This study aimed to improve acne treatment in women through the green synthesis of adapalene-conjugated silver nanoparticles using Moringa oleifera leaf extract, incorporated into an aloe vera gel.
Methods: The prepared adapalene-conjugated silver nanoparticles (ADN–AgNPs) were characterized for particle size, polydispersity index (PDI), and zeta potential (ζP) using dynamic light scattering, while physicochemical interactions were evaluated by Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), Brunauer–Emmett–Teller (BET) surface area analysis, and scanning electron microscopy (SEM). Entrapment efficiency (EE) and drug loading (DL) were quantified spectrophotometrically. In vitro release and antimicrobial activity were also assessed.
Results: The optimized formulation exhibited a mean hydrodynamic particle size of 228.5 nm, a polydispersity index of 0.502, and a zeta potential of −24.5 mV, indicating nanoscale particles with moderately broad size distribution and adequate colloidal stability typical of phyto-mediated green synthesis. FTIR spectra showed characteristic peak shifts confirming successful adapalene conjugation onto phytochemical-capped silver nanoparticles. X-ray diffraction analysis confirmed the formation of crystalline face-centered cubic silver nanoparticles, while additional peaks were attributed to phytochemical capping components. BET analysis demonstrated a high specific surface area (88.29 m²/g), while SEM micrographs showed quasi-spherical nanoparticles stabilized by phytochemical capping. The nanoparticles exhibited high entrapment efficiency (97.85%) and drug loading (48.92%). Incorporation into aloe vera gel produced a stable formulation with suitable pH, viscosity, spreadability, and uniform drug distribution. In vitro release studies showed significantly enhanced adapalene release (97.99±1.89% within 6 h), representing a 2.26-fold improvement over a marketed gel and following anomalous (non-Fickian) release kinetics governed by combined diffusion and polymer relaxation. Antimicrobial evaluation demonstrated strong inhibition against Escherichia coli (13±0.36 mm) and Staphylococcus aureus (16±0.14 mm), attributable to the collective contributions of silver nanoparticles, adapalene, and phytochemical constituents.
Conclusion: The developed ADN–AgNPs loaded aloe vera gel represents a promising eco-friendly, multifunctional topical delivery system offering enhanced drug release, antimicrobial efficacy, and therapeutic potential for acne management in women
INTEGRATED BIOANALYTICAL METHOD VALIDATION, PHARMACOKINETICS, AND METABOLITE CHARACTERIZATION OF 19‑MONOAMINOTHIAZOLE (19MAT): A CORRELATIVE IN‑SILICO AND IN‑VIVO STUDY USING LC–MS/MS
No full textObjective: This study is mainly focused on the development and validation of a robust liquid chromatography–tandem mass spectrometry (LC–MS/MS) method to accurately evaluate the pharmacokinetics (PK) and metabolite profile of 19‑Monoaminothiazole (19MAT), a newly synthesized compound showing promising antiviral activity against dengue virus (DENV). The work additionally integrated in‑silico metabolite prediction tools with experimental in‑vivo metabolite identification data to comprehensively understand the metabolic fate of 19MAT.
Methods: Triple‑quadrupole LC–MS/MS method was developed and validated as per ICH M10 (International council for harmonization of technical requirements for pharmaceuticals for human use) guidelines for its selectivity, linearity (1.27–1270 ng/mL), accuracy/precision, recovery, matrix effect, stability in rat plasma to quantify 19MAT to assess the PK after IV (Intravenous) and PO (Per oral) administration. Waters Xterra RP® C18 (150 mm × 4.6 mm, 5 μm) column was used in reverse phase separation of analyte and internal standard. Pharmacokinetics was assessed in Sprague Dawley rats (n=3 per dose group). BioTransformer 3.0 and SMARTCyp3.0 were used to predict metabolites, and a targeted LC–MS/MS strategy was used to identify the metabolites in plasma, urine, and feces.
Results: The assay showed linear response with r² > 0.99, recovery 48–63% with acceptable matrix factors, precision ≤~11% RSD (Relative standard deviation), and stability up to 45 days (−20/−70 °C). 19MAT exhibited rapid oral absorption (Tmax ≈ 0.42 h), moderate half‑life (PO: 4.20 h), high Vd (IV: ~1977 mL/kg), and bioavailability of 23.82%. Seven metabolites were identified via plasma, urine, and feces involving hydroxylation/dihydroxylation, O-dealkylation, and glucuronidation.
Conclusion: The integrated workflow establishes validated quantitation approach, appropriately identified pharmacokinetic properties, and maps metabolic pathways for 19MAT, supporting preclinical optimization
EVALUATION OF DIURETIC ACTIVITY OF ALCOHOLIC EXTRACT OF FLOWER BUDS OF NEOLAMARCKIA CADAMBA IN ALBINO RATS
No full textObjective: To study the diuretic activity of Alcoholic Extract of Flower buds of Neolamarckia cadamba by Lipschitz method in albino Wistar rats.
Methods: Metabolic cages were utilised to test the diuretic effect of Alcoholic Extract of Flower Buds of Neolamarckia cadamba in four Albino Wistar rats. Group I, the normal control, got vehicle (10 ml/kg or 1 ml of 0.9% NaCl/100 gm), group II received Frusemide (10 mg/Kg, p. o), and groups III and IV received low (200 mg/kg) and high (400 mg/kg) dosages of Alcoholic Extract of Neolamarckia cadamba flower buds Following Neolamarckia cadamba Alcoholic Extract treatment, rats were hydrated with saline (15 ml/kg, p. o) and put in metabolic cages at 25 °C±0.5 °C. Animals went 5 h without food or water. Each metabolic cage\u27s urine volume was assessed after 5 and 24 h. Total urine volume, ion concentration (Sodium, Potassium, Chloride), and pH were measured.
Results: In this model when compared to control group the Alcoholic Extract of Flower buds of Neolamarckia cadamba treated groups at different dose levels (200 and 400 mg/kg) have noted with significant increase in the urine volume and also significantly enhanced the excretion of Sodium, Potassium and Chloride ions in urine. In the urine pH no difference has been found.
Conclusion: Results showed that single dose administration of standard Furosemide and Alcoholic Extract of Flower buds of Neolamarckia cadamba significantly increased the urine output along with an increase in elimination of Sodium, Potassium, and Chloride ions. Alcoholic Extract of Flower buds of Neolamarckia cadamba, 400 mg/Kg produced a comparable diuretic activity with standard Frusemide
TREATMENT OPTIMIZATION IN RECURRENT DERMATOPHYTOSIS: A PROSPECTIVE, RANDOMIZED, COMPARATIVE STUDY OF EXTENDED-DURATION VERSUS HIGH-DOSE TERBINAFINE AND ITRACONAZOLE
No full textObjective: To compare efficacy and safety of terbinafine versus itraconazole administered in double dose and prolonged duration in patients with recurrent tinea corporis and cruris.
Methods: This prospective, randomized study included 166 patients in four groups: A (terbinafine 250 mg once daily (OD), 4 w), B (terbinafine 500 mg OD, 2 w), C (itraconazole 100 mg twice daily (BD), 4 w), and D (itraconazole 200 mg BD, 2 w). Primary outcomes were clinical/mycological cure, global assessment, safety; secondary outcomes included quality of life, escape treatment, adherence. Significance was set at p<0.05.
Results: Group C had highest efficacy (92.7% clinical cure and 100% mycological cure) with lowest recurrence. Liver Function Tests (LFTs) showed no significant abnormalities across all groups. No therapy discontinuations/serious Adverse Drug Reactions (ADRs) were reported. Dermatology Life Quality Index (DLQI) improved significantly from baseline to treatment end and 6 w post-treatment, indicating substantial and sustained improvement. Treatment compliance was high across all groups (≥90%), with no significant difference.
Conclusion: Itraconazole 100 mg BD for 4 w was most effective, well-tolerated regimen, highlighting benefit of extended duration over increased dose in recurrent dermatophytosis
A RANDOMIZED, DOUBLE-BLIND COMPARISON OF INTRATHECAL NALBUPHINE AND BUPRENORPHINE AS ADJUVANTS TO 1% 2-CHLOROPROCAINE FOR SPINAL ANESTHESIA IN AMBULATORY PERIANAL SURGERY
No full textObjective: Perianal surgeries in ambulatory settings require anesthetic agents with rapid onset, predictable duration, and minimal postoperative morbidity. This study compared the efficacy of Nalbuphine and Buprenorphine as intrathecal adjuvants to 1% 2-Chloroprocaine in spinal anesthesia for day-care perianal surgeries.
Methods: In this prospective, randomized, double-blind study, 68 ASA I/II patients aged 18–60 years undergoing elective perianal surgeries were randomized into two groups (n=34 each). Group B received 40 mg 1% 2-Chloroprocaine+Buprenorphine 60 μg; Group N received 40 mg 1% 2-Chloroprocaine+Nalbuphine 0.4 mg. Outcomes included onset and duration of sensory and motor blocks, regression times, postoperative analgesia, hemodynamic stability, and adverse effects.
Results: Sensory block onset was faster in Group B (2.6±1.28 min) compared to Group N (3.71±1.0 min, p<0.001). Motor block onset was also faster with Buprenorphine (2.85±1.23 min vs 3.71±1.0 min, p<0.01). Nalbuphine prolonged regression to S2 (71.29±8.66 min vs 66.82±9.27 min, p<0.001) and duration of motor block (64.41±7.86 min vs 59.65±9.74 min, p<0.05). Time to rescue analgesia was longer with Nalbuphine. Hemodynamics remained stable; adverse effects were minimal.
Conclusion: Intrathecal Buprenorphine and Nalbuphine are safe and effective adjuvants to 1% 2-Chloroprocaine for spinal anesthesia in day-care perianal surgeries. Buprenorphine ensures faster onset of block, while Nalbuphine provides superior and longer-lasting postoperative analgesia. Both support early ambulation and discharge, making them valuable options in ambulatory anesthesia