Innovare Academic Sciences: E-Journals
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FACTORS INFLUENCING FOOD TOURISM IN QIANXINAN PREFECTURE
No full textFood is a reflection of culture, and culinary tourism is considered a branch of cultural tourism. It is a form of tourism that focuses on enjoying food and emphasizes the use of food-related resources as attractions. Culinary tourism provides tourists with memorable experiences through its unique food consumption value while directly or indirectly influencing the destination’s image. In existing research, most studies on factors affecting tourism motivation have focused on analyzing the relationship between tourism motivation and tourists, or between tourism motivation and tourism destinations, lacking articles discussing the relationships among all three. Therefore, taking Qianxinan Prefecture as an example, this study collects information through interviews and observations by dividing the research subjects into three dimensions (subject, object, and intermediary) to analyze the factors influencing tourists’ food tourism motivation and the connections between these factors. Through descriptive analysis of the relationships between various dimensions and factors, this thesis constructs a relationship model, revealing the cyclical and holistic nature of these factors, and uses this model to explore issues arising at various stages of culinary tourism development
DESIGN, SYNTHESIS, AND EVALUATION OF NOVEL TYROSINASE INHIBITORS FOR SKIN DEPIGMENTATION
No full textObjective: Hyperpigmentation is a prevalent dermatological condition caused by excessive melanin production, primarily catalyzed by the enzyme tyrosinase. Existing depigmenting agents, such as hydroquinone and kojic acid, are limited by cytotoxicity, instability, and suboptimal efficacy. This study aimed to design, synthesize, and evaluate structurally novel tyrosinase inhibitors derived from cinnamic acid to overcome these limitations.
Methods: Tencinnamic acid-based derivatives were designed with strategic modifications, including esterification with hydroquinone and aromatic moieties, to enhance binding affinity and stability. Molecular docking studies were conducted using tyrosinase crystal structures (PDB IDs: 3NQ1 and 5I38) to identify key binding interactions. Six lead compounds were synthesized and structurally characterized via NMR and FTIR spectroscopy. Their tyrosinase inhibitory activity was assessed in vitro using mushroom tyrosinase under standardized assay conditions.
Results: Molecular docking revealed favorable interactions within the tyrosinase active site, with compound 9 exhibiting the highest docking scores. In vitro assays confirmed compound 9 as the most potent inhibitor, with an IC₅₀ value of 31.35 µg/ml, outperforming kojic acid (IC₅₀ = 94.96 µg/ml) and hydroquinone (IC₅₀ = 772.8 µg/ml) under identical conditions.
Conclusion: Compound 9 demonstrated superior tyrosinase inhibition compared to conventional agents, indicating its potential as a safer and more effective alternative for treating hyperpigmentation. These findings support further development of compound 9 for use in topical formulations targeting melasma and related pigmentary disorders, with planned follow-up studies including in vivo efficacy and safety evaluations
PREPARATION AND EVALUATION OF A CHITOSAN HYDROGEL-BASED SLOW-RELEASE SYSTEM LOADED WITH DOCETAXEL AND EUPHORBIA MICROSCIADIA FOR BREAST CANCER THERAPY IN A MURINE MODEL
No full textObjective: To develop and evaluate a thermosensitive chitosan hydrogel co-loaded with docetaxel and a standardized E. microsciadia extract for breast cancer treatment in a murine 4T1 model.
Methods: The aerial parts of E. microsciadia were collected and identified. A chitosan hydrogel was prepared and loaded with docetaxel and Euphorbia extract. The morphological characteristics of the hydrogel were evaluated using scanning electron microscopy (SEM). Subsequently, the in vitro release profiles of docetaxel and Euphorbia extract from the hydrogel were determined. The antitumor efficacy of the prepared hydrogels was assessed in tumor-bearing mice by monitoring tumor size reduction, followed by histopathological examination of excised tumor tissues.
Results: SEM confirmed hydrogel crosslinking with 5–10 µm pore sizes versus 10–20 µm in controls. Initial release of 60% of both agents occurred within 10 h, reaching 80% by 72 h. Docetaxel and E. microsciadia significantly reduced tumor volumes compared to control (p<0.001). The combination treatment showed no significant difference from docetaxel alone (p>0.05), suggesting no synergistic effect. Histology revealed that combination therapy (docetaxel+E. microsciadia) exhibited superior tumor suppression, with significant cell degeneration and necrosis compared to other treatments.
Conclusion: The co-loaded thermosensitive chitosan hydrogel provides controlled release and effective in vivo antitumor activity. Lack of synergy warrants further optimization to enhance clinical relevance versus current docetaxel systems
MIXED MICELLES: ADVANCED NANOCARRIERS FOR PULMONARY MUCOLYTIC DRUG DELIVERY-A SYSTEMATIC SCOPING REVIEW
No full textThis study is to summarize and analyze existing materials on advanced mixed micellar systems for the pulmonary transmission of mucolytic drugs. This review focuses on the composition and preparation of these compounds, their performance characteristics, and key obstacles slowing down clinical use for mucoreactive respiratory diseases. A systematic scoping a review of the scientific literature was conducted using PubMed and Scopus. We also searched in Embase. This review encompassed all sources from 2000 to 2024. Our searching strategy used key information related to mixed micelles, nanocarriers, delivery to lungs, mucolytics, and performance parameters. The review included original research papers, comparative studies, and other relevant reviews. Mixed micelles, which are usually 10 nm-100 nm in size, are conducive to pulmonary drug delivery. Combining polymers (e. g., Pluronics®) and surfactants (e. g., TPGS) results in high thermodynamic stability (low critical micelle concentration), high encapsulation efficiency for hydrophobic mucolytics like bromhexine HCl, and favorable mucus penetration. This is because of their small size and highly modifiable PEGylated surfaces. Thin-film hydration is a common method for preparing mixtures. Compared with liposomes, mixed micelles offer increased stability during nebulization and easier and more scalable manufacturing methods. Mixed micelles are a promising and highly adaptable nanocarrier system designed for delivering mucolytic agents to the lungs, as they facilitate significant elimination of mucus. The workable evidence from preclinical studies is strong. However, major translational gaps remain. Future research must be able to optimize systematically the formulations for specific mucolytics and carry out long-term safety and efficacy studies in vivo within relevant disease models. Researchers need to build the infrastructure for scalable, GMP-compliant production of these products to realize their potential to save lives
PREPARATION AND IN VITRO EVALUATION OF BUTENAFINE HCL NANOSUSPENSION
No full textObjective: One of the significant problems associated with poorly soluble drugs is low bioavailability. Butenafine HCl is classified as BCS Class II by the biopharmaceutical classification system, with low solubility and high permeability. Objectives: Formulation as a nanosuspension is an attractive and promising alternative to solve low solubility problems and low bioavailability
Methods: A nanosuspension of Butenafine HCL was generated utilizing a bottom-up method through the solvents/anti-solvents procedure characterized by particle size analysis, polydisperse index, and entrapment efficacy, and then the selected formula was described by dissolution testing, differential scanning calorimetry, X-ray powder diffraction, FTIR, and FESEM. Nanosuspensions were prepared via the solvent/anti-solvent procedure, using different polymer types and ratios.
Results: Butenafine solubilized in PBS with 1% soluplus, PVP, PEG 400, and poloxamer was 14.32±0.011, 6±0.01, 10.48±0.012, and 2.025±0.001. To form a nanosuspension with particle sizes ranging from 78 to 516 ±0.01 nm, entrapment up to 96%, and a Drug content of 99%. Particle size of optimum formula, consisting of Butenafine HCL and soluplus® in a ratio of drug: stabilizer (Soluplus®):co-stabilizer (PEG400) is (1:8:2.5) measured in nanostructure, and it was equal to 78.3±0.03 with a PDI 0.2511±0.13, which is in the nanosized range, drug content of optimum formula 99.6±0.013, and entrapment was 96±0.012. Osmolarity adjusted to a range of 280 to 310 mOsm/Kg. The release of the drug after 120 min was 95%. FTIR spectra show a distinct peak for the drug, indicating no chemical interaction between BF and Soluplus®. DSC shows a slight shift in the melting point to 220.50 °C due to the presence of cryoprotectants. PXRD shows amorphous formation due to nanosuspension, and FESEM shows the size and shape of the nanosuspension, in which the size of the particle by FESEM was 72.9 nm, which is close to the measured particle size. The stability study of the optimal formula after three months showed a particle size of 78 nm at 5 °C and 80 nm at 25 °C.
Conclusion: Using soluplus as a stabilizer at various concentrations successfully produced a nanosuspension of Butenafine HCl. The best formula, consisting of Butenafine HCL and soluplus® in a ratio of drug: stabilizer (Soluplus®):co-stabilizer (PEG400) is 1:8:2.5
MIRTAZAPINE LOADED PRONANOMICELLES: PREPARATION AND CHARACTERIZATION
No full textObjective: The aim of this work was to prepare mirtazapine-loaded self-assembled micelles using soluplus®, solutol®HS15 and TPGs to enhance mirtazapine solubility and thus oral bioavailability.
Methods: MTZ nanomicelles were produced by the thin-film hydration method using different polymers in different ratios to prepare stable MTZ nanomicelles, where the soluplus® nanomicelles formula in different ratios was F1 to F4; soluplus® in combination with TPGS to stabilize the nanomicelles formula was formulated in different ratios as in F5 to F10; and soluplus® in combination with SolutolHS 15 as in F10 to F14. The most stable formula is further investigated with particle size, polydispersity index, drug loading, entrapment efficacy, and in vitro release, and then the selected formula is statistically further investigated with FTIR, DSC, and FESEM.
Results: The particle size of the prepared formula ranged from 57 nm for F4 (1:10 of MTZ: soluplus®) to 78 nm for F8 (1:8:4 of MTZ: soluplus®: TPGS); the EE% ranged from 85% to 90%; FTIR analysis suggested no chemical interaction; FESEM showed spherical nanomicelles in Nano size; and DSC showed the transition of the drug to an amorphous form due to MTZ entrapment with in nanomicelles.
Conclusion: Mirtazapine-loaded Soluplus® micelles alone and in combination, first with TPGS and second with Solutol HS 15 by the thin-film hydration method show uniform distribution of particle size, PDI, and enhancement in the in vitro release of the drug
FORMULATION AND OPTIMIZATION OF FLOATING SUSTAINED RELEASE TABLETS OF RITONAVIR THROUGH BOX-BEHNKEN DESIGN
No full textObjective: The purpose of this study is to design and evaluate floating sustained-release tablets of ritonavir (RTZ) employing box-behnken development (BBD).
Methods: The BBD was utilized to improve the formulation parameters. The main release-retarding polymers were selected as independent variables: methocel K100M (A), the gas-generating agent was sodium bicarbonate (B), the secondary release-retarding polymer was ethyl cellulose (C), and the floating aid was Cetyl alcohol and which was kept constant. Floating lag time (FLT) (Y1), swelling index (SI) (Y2), and percentage drug release (Y3) were chosen as the dependent variables. Differential scanning calorimetry (DSC) and fourier transform infrared spectroscopy (FTIR) were used to assess the compatibility of the drug and excipient. FLT, flotation time, SI, hardness, drug content, friability, in vitro drug release, and drug release kinetics were assessed after the tablets were manufactured using the direct compression method.
Results: FTIR and DSC analyses showed no interaction between the drug and the excipients. Every tablet that was tested produced positive outcomes. The validated optimized (VO) tablets exhibited zero-order kinetics, with a steady and sustained drug release over 12 h (95.76±0.75 %), FLT of VO formulation was found to be 53±0.5 sec with 91.21±1.6% of SI. In vivo bioavailability of optimized formulation shows a 1.5-fold increase in bioavailability.
Conclusion: Using a statistical optimization model, the optimized tablets with the desired formulation characteristics were identified. The optimized formulation remarkably maintained the drug release for up to 12 h, suggesting improved therapeutic potential for HIV therapy
DENDRIMERS IN OCULAR DRUG DELIVERY: A COMPREHENSIVE REVIEW
No full textThe anatomical and physiological complexity of the eye significantly hinders drug delivery to both the anterior and posterior segments, complicating the treatment of various ocular diseases. Although conventional ophthalmic formulations, primarily topical eye drops, are widely used, their bioavailability remains low. Recent advancements in nanotechnology have introduced dendrimers as promising nanoscale drug carriers for ocular therapy. Dendrimers can enhance drug solubility, permeability, stability, and retention owing to their unique branched architecture, multivalent surface functionality, and capacity for precise drug targeting. This review discusses the anatomical barriers to ocular drug delivery, innovative strategies to overcome them, and highlights various dendrimer generations, types, synthesis methods, and their applications in treating eye disorders such as glaucoma, age-related macular degeneration, diabetic retinopathy, and uveitis. Furthermore, it explores clinical studies, patents and their ocular applications/rationale, and regulatory hurdles associated with the clinical translation of dendrimer-based therapeutics. Despite, promising preclinical data, manufacturing and regulatory challenges remain major hurdles for their widespread clinical use. Dendrimers hold great promise as advanced ocular drug delivery systems, with the potential to improve treatment efficacy for a wide range of vision-impairing disorders
EXPERIMENTAL SOLID DISPERSION APPROACH TO ENHANCE THE SOLUBILITY AND THERAPEUTIC PERFORMANCE OF DOLUTEGRAVIR
No full textObjective: Dolutegravir (DTG), an HIV-1 integrase strand transfer inhibitor (INSTI), shows poor aqueous solubility (~15 µg/ml), limiting its therapeutic performance. This study aimed to enhance DTG solubility and oral bioavailability using various solid dispersion techniques.
Methods: Solid dispersions (SDs) were prepared by five methods-physical mixing, co-grinding, kneading, rota solvent evaporation, and lyophilization-using nine carriers: mannitol, PEG 4000 (polyethylene glycol 4000), PVP K90 (polyvinylpyrrolidone), HPMC E5LV (hydroxypropyl methylcellulose), Captisol®, Gelucire 44/14, Poloxamer 188, Poloxamer 407, and Soluplus® at drug-to-carrier ratios of 1:1–1:4 (w/w). Formulations were evaluated for solubility, dissolution, and in vivo pharmacokinetics in New Zealand white (NZW) rabbits using validated HPLC methods.
Results: Among 24 formulations, Lyophilization with Soluplus® and Captisol yielded the highest dissolution rates, with 89.14±1.17% and 77.14±1.63% drug release after 2 h. This marked improvement over pure DTG (14.63±0.72% release) was attributed to the effective conversion of the crystalline drug to an amorphous state and the formation of a homogeneous dispersion. Soluplus® demonstrated superior performance in enhancing DTG solubility and dissolution rate compared to Captisol. The solid dispersion formulation demonstrated superior pharmacokinetic properties compared to both the Dolutegravir and the marketed formulation. At 2 h post-administration, the mean plasma concentration for the F24 was 3236.71±461.42 ng/ml, compared to 1457.42±221.54 ng/ml for Dolutegravir and 2465.85 ±456.23 ng/ml for the marketed formulation.
Conclusion: Lyophilization with Soluplus® significantly enhanced solubility, dissolution, and oral bioavailability of DTG, providing a promising strategy for improved oral delivery. The experimental results collectively confirm that lyophilization with Soluplus® is a reproducible and scalable approach for solubility enhancement of dolutegravir
EMERGING NOSE-TO-BRAIN DRUG DELIVERY STRATEGIES FOR AMYOTROPHIC LATERAL SCLEROSIS: A PROMISING FRONTIER IN NEUROTHERAPEUTICS
No full textThe progressive neurodegenerative illness known as amyotrophic lateral sclerosis is characterized by the death of motor neurons, which causes paralysis, muscle atrophy, and ultimately fatal respiratory failure. Despite advances in understanding its molecular pathology, currently approved therapies such as Riluzole and Edaravone offer only modest clinical benefits, largely due to limited central nervous system exposure. The blood–brain barrier remains a major challenge for effective drug delivery to neural targets. In this context, intranasal nose-to-brain delivery has emerged as a promising non-invasive strategy to bypass the blood–brain barrier via olfactory and trigeminal neural pathways, enabling direct drug transport to the brain while reducing systemic exposure. Recent preclinical studies have explored a range of nanocarrier-based systems, including polymeric nanoparticles, lipid-based carriers, nanoemulsions, and hybrid formulations, to enhance nasal residence time, epithelial uptake, and neuronal transport. Functionalization with targeting ligands and mucoadhesive components has further improved brain targeting efficiency and therapeutic retention. However, challenges related to formulation complexity, long-term safety, scalability, and clinical translation remain unresolved. This review critically evaluates recent advances in nanocarrier-mediated nose-to-brain delivery for amyotrophic lateral sclerosis, highlighting current limitations and future directions required for successful clinical application