Cumulative Drug Research Articles

Microemulgel Delivery of Ciprofloxacin Hydrochloride

Background: Ciprofloxacin hydrochloride is broad spectrum carboxyfluoroquinolone antibiotic from biopharmaceutics classification system (BCS) class IV. The oral dosage form exhibits gastric irritation whereas the topical cream has demonstrated poor penetration and low bioavailability. Objective: To optimize microemulsion-based gel of ciprofloxacin hydrochloride to increase its solubility and permeability through the cutaneous layer for targeting bacterial skin infections. Methods: To develop microemulsion, oil (soya oil, castor oil, oleic acid, isopropyl myristate and vegetable oil), surfactant (cremophore, span 80, tween 80) and cosurfactant (PEG 600 and PEG 400, propylene glycol) were evaluated. To depict the microemulsion formulation pseudo ternary phase diagram was employed. %Transmittance, zeta potential, dissolution study and size analysis were carried out for evaluation of microemulsion. 32 factorial design was used. Two variables i.e concentration of Sepineo P600 and Carbopol 934 effect on microemulgel was evaluated. Evaluation of gel was carried for physical parameters, antimicrobial, in-vitro and ex-vivo release study. Results: Solubility analysis suggested tween 80, oleic acid and propylene glycol for the formulation of microemulsion. Zeta potential for microemulsion batch F1 was -11.3 mV. This indicated good stability. In-vitro release study showed 91.98% percentage cumulative drug release for batch F1 at 8 hours. Microemulsion-based gel (F1) showed 22.96% inhibition against bacteria which proved its antibacterial activity. Conclusion: The obtained results exhibited that the permeability and bioavailability of the drug was increased when given through a topical route.

Formulation Development and Evaluation of Herbal Antifungal Cream by using Psidium guajava Leaf Extract

Fungal infection is one of the major health concerns globally and varies from superficial to systemic infections. Psidium guajava Linn. leaf extract showed antifungal activity against wide range of fungi. The present research focuses on the development and investigation of cream with guava leaf extract. Ethanolic, methanolic and hydroalcoholic leaf extract was evaluated for total flavonoid content, thin layer chromatography (TLC), high-performance thin layer chromatography (HPTLC) and antifungal activity against Candida albicans. Further cream-based extract was optimized using 32 factorial designs. Beeswax and tween 80 were selected as the independent variables whose impact was studied on viscosity and %cumulative drug diffusion. Optimized cream was characterized by appearance, pH, washability, spreadability, in-vitro drug diffusion study, antifungal test and skin irritation test on wistar rats. The hydroalcoholic extract showed the highest content of flavonoids and a better zone of inhibition (27 ± 1 mm). HPTLC results confirmed the presence of essential flavonoids. Cream with 6% beeswax and 5% tween 80 with a viscosity 10420 cP and 70% drug diffusion was considered as optimized batch. The prepared cream showed satisfactory results for all evaluated parameters. The antifungal test showed the highest zone of inhibition for cream (25 mm) in comparison to standard formulation (23 mm). No any sign of skin irritation was observed. The prepared formulation is the best suitable alternative for the available topical antifungal formulation

Olmesartan Medoxomil-Loaded Niosomal Gel for Buccal Delivery: Formulation, Optimization, and Ex Vivo Studies.

Olmesartan medoxomil (OLM) is a low bioavailability antihypertensive drug. This study aimed to prepare and optimize an OLM niosomal gel and investigate drug permeation via a chicken buccal pouch. OLM-loaded niosome were prepared using a film hydration technique. The vesicle size, zeta potential, entrapment efficiency, and percentage cumulative drug release of niosome were evaluated. The niosomes were incorporated into a Carbopol 974P (1.5% w/v) gel, and the drug permeability of the niosomal gel was evaluated. The formulations of the niosomal gel were optimized using the Box-Behnken design. The optimized formulation was further characterized by transmission electron microscopy (TEM) and Fourier transform infrared radiation analysis. The particle size and zeta potential of the optimized niosomal formulations were 296.4 nm and -38.4 mV, respectively. Based on TEM analysis, the niosomes were found to be spherical in shape. The permeability, flux, and permeability coefficient of the optimized niosomal gel were 0.507 mg/cm2, 0.083 mg/cm2 × hour, and 041 cm/hour, respectively. Histopathological evaluation revealed that the niosomal gel had better permeability than the OLM gel. Based on the results of the OLM niosomal gel, it can be concluded that the formulation can be beneficial in increasing bioavailability, resulting in better therapeutic efficacy.

Development of microemulgel formulations with varied permeation enhancers for transungual delivery of luliconazole in onychomycosis management

Luliconazole-loaded microemulgels containing different permeation enhancers were formulated for transungual drug delivery for the management of onychomycosis, onychomycosis, which affects nails. The physicochemical properties like droplet size, zeta potential, pH, viscosity, spreadability, extrudability, oil binding capacity, drug content, and microscopic study were evaluated. The Pseudo-ternary phase diagram was constructed for the formulation of microemulsions (MEs) by keeping the Km ratio constant at 3:1 and characterized for clarity, mean droplet size, zeta potential, viscosity, pH, transmittance, refractive index, and stability. The ME mean droplet size and zeta potential were found in the range of 38.78 to 171.4 nm, and 0.00 to − 6.6 mV, respectively. Prepared MEs were converted into microemulgel by adding a 2.5% gelling agent (Carbapol 934) in the external phase, and a drug release study was conducted. Formulation E3 showed better drug release and was chosen as the control. Four different penetration enhancers were added separately within E3 and further evaluated for pH, viscosity, spreadability, extrudability, oil binding capacity, drug content, microscopic study, Compatibility study, XRD, and DSC. A favorable docking score was observed between luliconazole and Lanosterol 14-alpha-demethylase. In-vitro cumulative drug release at the end of 24 h from E3-SS, containing sodium sulfide as a penetration enhancer, was found to be 94.70% and was 2 times more than the control formulation. Ex-vivo transungual permeation studies through cutting nail clippings were found to be in the range of 28.18 - 36.52 µg/mm2. The microemulgels tagged as E3, E3-SS, and E3-SL showed a significant zone of inhibition against Candida albicans and Aspergillus fumigatus as compared to the marketed formulation.

Formulation Development and In-Vitro Evaluation of Transferosomal Gel of Mometasone Furoate

The main aim of the study is to formulate and evaluate transferosomal gel formulation for effective topical delivery of Mometasone furoate. The transferosomes was prepared using thin film hydration technique by various proportions of Soya phosphatidylcholine, tween 80. The drug was encapsulated into eight different Transferosomal formulations from F1-F8. The optimized formulation F4 showed small particle size (152.48 nm), entrapment efficiency % EE of 87.16%, zeta potential of -32mV, 0.252 PDI and % Cumulative Drug Release of (97.14%). SEM of optimized Transferosome appeared as spherical, well identified, Unilamellar vesicles. The optimized formulation of Transferosomes was further formulated to transferosomal gel with Carbopol-940 (0.2 to 0.8% w/w), HPMC k15 (0.2 to 0.8% w/w), Propylene glycol, Triethanolamine and Isopropyl alcohol. Among these, F4 formulation with Carbopol-940 0.8%w/w transferosomal gel is the optimized transferosomal gel and showed Spreadability value 0.229±0.01gm.cm/sec, pH value 5.8. The actual drug content of the Transferosomal gel was found to be 98.90%, which represents good content uniformity. The viscosity of optimized Transferosomal gel was found to 55417cps. The percentage drug release for Transferosomal gel was 98.22%. And the formulation was stable throughout the stability studies. This research suggests that Mometasone Furoate loaded transferosomal gel can be potentially used as a transdermal drug delivery system for effective topical delivery.
 Keywords: Mometasone Furoate, Transfersomes, Soya phosphatidyl choline and Tween 80.

Efficient and Traceable Tamoxifen Delivery to Breast Cancer Cells Using Folic Acid‐Decorated and PEGylated Graphene Quantum Dots

AbstractGraphene quantum dots (GQDs) possess potential properties for the targeted transport and tracking of anticancer medication to tumor cells. For this purpose, the synthesized GQDs were decorated with folic acid (FA) and methoxy polyethylene glycol (mPEG2000), and finally loaded with tamoxifen (TMX) drug. The synthesized nano‐drug was characterized using FTIR, XRD, UV‐Vis, PL, HRTEM, FESEM, and DLS analytical devices. Based on the obtained data, the average hydrodynamic diameter of particles dissolved in water was 294.7 nm and the size of dehydrated particles was between 53 and 210 nm. PL data showed that prepared nanoparticles have an emission wavelength of 438 nm, which is in the blue fluorescent wavelength range, thus making these nanoparticles suitable for cell imaging. The encapsulation efficiency and loading percentage of tamoxifen in nanoparticles were calculated at about 52.5 % and 30 %, respectively, and cumulative drug release reached 89 % within 42 hours. The cytotoxicity effects of nanoparticles were investigated. According to IC50 results, the targeted mPEG‐GQDs‐FA/TMX (TMX‐FPGs) nano‐drug was more toxic than free TMX on MCF‐7 cells and had reduced side effects on healthy HDF cells. TMX‐FPGs induced apoptosis cell death, significantly. The confocal imaging experiments showed that TMX‐FPGs are appropriate for monitoring and targeting MCF‐7 cells.

Design and evaluation of antibacterials crosslinked chitosan nanoparticle as a novel carrier for the delivery of metronidazole to treat bacterial vaginosis

Bacterial vaginosis (BV) is a recurring, chronic infection that is difficult to treat due to the limited bioavailability of antimicrobials within vaginal epithelial cells. Vaginal administration, because of lower dosing and systemic exposure offers a viable option for treating vaginal infections. In this study, Metronidazole-loaded chitosan nanoparticles were synthesised employing borax (BX) or tannic acid (TA) as an antimicrobial crosslinking agent for treating BV. The prepared NPs were characterized for various physical, physicochemical, pharmaceutical, thermal and antibacterial properties. Morphological investigation revealed that nanoparticles prepared from 0.5 % w/v chitosan, 1.2 % w/v BX, and 0.4 % w/v metronidazole (MTZ) were non-spherical, with particle sizes of 377.4 ± 37.3 nm and a zeta potential of 34 ± 2.1 mV. The optimised formulation has MIC values of 24 ± 0.5 and 59 ± 0.5 μg/mL, against Escherichia coli (E.coli) and Candida albicans (C.albicans) respectively. The results of DSC and XRD demonstrated no change in the physical state of the drug in the finished formulation. Under simulated vaginal fluid, the optimised formulation demonstrates a cumulative drug release of about 90 % within 6h. The prepared borax crosslinked NPs exhibit anti-fungal activities by inhibiting ergosterol synthesis. The in-vivo antibacterial data indicated a comparable reduction in bacterial count compared to the marketed formulation in female Swiss albino mice treated with optimised nanoparticles. According to histopathological findings, the prepared nanoparticle was safe for vaginal use. Based on the experimental findings, it was concluded that MBCSNPs, due to their good physiochemical and antimicrobial properties, could serve as a potential topical alternative for treating BV and reducing fungal infection.

Development and evaluation of a protease inhibitor antiretroviral drug-loaded carbon nanotube delivery system for enhanced efficacy in HIV treatment

The primary objective of this study was to enhance the effectiveness of the protease inhibitor antiretroviral drug by designing a novel delivery system using carboxylated multiwalled carbon nanotubes (COOH-MWCNTs). To achieve this, Fosamprenavir calcium (FPV), a prodrug of amprenavir known for inhibiting the proteolytic cleavage of immature virions, was selected as the protease inhibitor antiretroviral drug, and loaded onto COOH-MWCNTs using a direct loading method. The structural specificity of the drug-loaded MWCNTs, the percent entrapment efficiency, and in vitro drug release were rigorously evaluated for the developed formulation, referred to as FPV-MWCNT. Fourier transform infrared (FTIR) spectroscopy, Field emission scanning electron microscopy (FE-SEM), Raman spectroscopy, and atomic force microscopy (AFM) techniques were employed to confirm the structural integrity and specificity of the FPV-MWCNT formulation. The results demonstrated a remarkable entrapment efficiency of 79.57 ± 0.4 %, indicating the successful loading of FPV onto COOH-MWCNTs. FE-SEM and AFM analyses further confirmed the well-dispersed and elongated structure of the FPV-MWCNT formulation, without any signs of fracture, ensuring the stability and integrity of the drug delivery system. Moreover, particle size analysis revealed an average size of 290.1 nm, firmly establishing the nanoscale range of the formulation, with a zeta potential of 0.230 mV, signifying the system's colloidal stability. In vitro drug release studies conducted in methanolic phosphate buffer saline (PBS) at pH 7.4 and methanolic acetate buffer at pH 5 demonstrated sustained drug release from the FPV-MWCNT formulation. Over a period of 96 h, the formulation exhibited a cumulative drug release of 91.43 ± 2.3 %, showcasing the controlled and sustained release profile. Furthermore, hemolysis studies indicated a notable reduction in the toxicity of both FPV and MWCNT upon conjugation, although the percent hemolysis increased with higher concentrations, suggesting the need for careful consideration of dosage levels.In conclusion, the findings from this study underscore the potential of the FPV-MWCNT formulation as an effective and promising drug-conjugated system for delivering antiretroviral drugs. The successful encapsulation, sustained drug release, and reduced toxicity make FPV-MWCNT a compelling candidate for enhancing the therapeutic efficacy of protease inhibitor antiretroviral drugs in the treatment of HIV. The developed delivery system holds great promise for future advancements in HIV treatment and paves the way for further research and development in the field of drug delivery utilizing carbon nanotube-based systems.

Injectable, rapid self-healing, antioxidant and antibacterial nanocellulose-tannin hydrogels formed via metal-ligand coordination for drug delivery and wound dressing

Nanocellulose-based hydrogels have attracted increasingly attention due to their biocompatibility, biodegradability, and hydrophilic properties. In this work, we proposed a simple route to fabricate composite hydrogels using TEMPO oxidized cellulose nanofibrils (TOCNF) and tannin through metal-ligand coordination. Calcium ions were utilized to rapidly cross-link the carboxyl groups on TOCNF and the tannins' catechol moieties via metal-ligand bonding, resulting in the formation of TOCNF-Ca2+-T composite hydrogels. The incorporation of tannins endowed the hydrogel with high antioxidant and antibacterial properties. The rheological analysis revealed that the addition of tannin led to an improved gel strength of the composite hydrogel. The hydrogel was injectable and could autonomously self-healed in 1 min without any trigger. Tetracycline hydrochloride (TH) was successfully loaded into the composite hydrogels, achieving a maximum encapsulation rate of 97.32%. TOCNF-Ca2+-40%T demonstrated a cumulative drug release of 36% at pH 1.3 and 86% at pH 7.4, indicating its pH-responsive nature. These hydrogels, derived from plant sources, exhibited high antibacterial and antioxidant properties, as well as biocompatibility, rapid self-healing, and injectability, which open up new possibilities for applications in wound dressing and drug delivery.

Association of anticholinergic drug exposure with the risk of dementia among older adults in Japan: The LIFE Study.

Several studies have investigated that anticholinergic drugs cause cognitive impairment. However, the risk of dementia associated with anticholinergics has not been extensively investigated in the super-aging society of Japan. We conducted this study to assess the association between anticholinergic drugs and the risk of dementia in older adults in Japan. This nested case-control study used data from the Longevity Improvement & Fair Evidence Study, which includes claim data in Japan from 2014 to 2020. We included 66,478 cases of diagnosed dementia and 328,919 matched controls aged ≥65years, matched by age, sex, municipality, and cohort entry year. Primary exposure was the total cumulative anticholinergic drugs prescribed from cohort entry date to event date or matched index date, which was the total standardized daily doses for each patient, calculated by adding the total dose of different types ofanticholinergic drugs in each prescription, divided by the World Health Organization-defined daily dose values. Odds ratios for dementia associated with cumulative exposure to anticholinergic drugs were calculated using conditional logistic regression adjusted for confounding variables. The mean (standard deviation) age at index date was 84.3 (6.9), and the percentage of women was 62.1%. From cohort entry date to event date or matched index date, 18.8% of the case patients and 13.7% of the controls were prescribed at least one anticholinergic drug. In the multivariable-adjusted model, individuals with anticholinergic drugs prescribed had significantly higher odds of being diagnosed with dementia (adjusted odds ratio, 1.50 [95% confidence interval, 1.47-1.54]). Among specific types of anticholinergic drugs, a significant increase in risk was observed with the use of antidepressants, antiparkinsonian drugs, antipsychotics, and bladder antimuscarinics in a fully multivariable-adjusted model. Several types of anticholinergic drugs used by older adults in Japan are associated with an increased risk of dementia. These findings suggest that the underlying risks should be considered alongside the benefits of prescribing anticholinergic drugs to this population.

Cachexia Prevalence in a Population of Moroccan Women with Rheumatoid Arthritis.

To assess body composition in women with rheumatoid arthritis (RA) compared to healthy controls, to calculate the prevalence of rheumatoid Cachexia (RC), and to identify the associated factors. We conducted a case-control study on 112 female patients with RA according to the 2010 American College of Rheumatology/European League Against Rheumatism classification criteria for RA; and 224 age-matched healthy women. Body composition (BC) and bone mineral density (BMD) scans were obtained using Dual-energy X-ray absorptiometry (DXA). RC was defined by a fat-free mass index (FFMI) below the 10th percentile and a fat mass index (FMI) above the 25th percentile compared with the control group. We conducted a comparison between RA patients and healthy controls then a multiple regression analysis was conducted where the dependant variable is the presence of RC. RC prevalence was 42.85% while the mean body mass index (BMI) was the same in both groups. RA patients had a higher FM and lower FFM comparing to healthy controls. In our population, 78.60% of patients were on methotrexate and 12.50% on anti TNF therapy. Comparison between patients with and without RC showed that patients with RC have a higher proportion of erosive arthritis and of active disease. Regression logistic analysis showed that RC was significantly associated to erosive arthritis and active disease (OR at 33.31 (8.42-131.70) and 8.98 (1.64-49.20) respectively), independently of age, erythrocyte sedimentation rate, C-reactive protein, disease duration, steroid cumulative dose and biologic Disease-Modifying Anti-Rheumatic Drugs(bDMARDs) use. Our study showed that almost half of our RA patients have RC, even with a high BMI.

Augmentin loaded functionalized halloysite nanotubes: A sustainable emerging nanocarriers for biomedical applications

Clay minerals such as Halloysite nanotubes (HNTs), abundantly available green nanomaterial, exhibit a significant advantage in biomedical applications such as drug delivery, antibacterial and antimicrobials, tissue engineering or regeneration, etc. Because of the mesoporous structure and high absorbability, HNTs exhibit great potential as a nanocarrier in drug delivery applications. The sulfuric acid treatment enhances the surface area of the HNTs and thereby improves their drug-loading capacity by enlarging their lumen space/inner diameter. In the present investigation, based on the literature that supports the efficacy of drug loading after acid treatment, a dual treatment was performed to functionalize the HNTs surface. First, the HNTs were etched and functionalized using sulfuric acid. The acid-functionalized HNTs underwent another treatment using (3-aminopropyl) triethoxysilane (APTES) to better interact the drug molecules with the HNTs surfaces for efficient drug loading. Augmentin, a potential drug molecule of the penicillin group, was used for HNTs loading, and their antibacterial properties, cytotoxicity, and cumulative drug release (%) were evaluated. Different characterization techniques, such as X-ray diffractometer (XRD) and Fourier Transform Infra-Red (FT-IR), confirm the loading of Augmentin to the APTES@Acid HNTs. TEM images confirm the effective loading of the drug molecule with the HNTs. The drug encapsulation efficiency shows 40.89%, as confirmed by the Thermogravimetric Analysis (TGA). Also, the Augmentin-loaded APTES@Acid HNTs exhibited good antibacterial properties against E. coli and S. aureus and low cytotoxicity, as confirmed by the MTT assay. The drug release studies confirmed the sustainable release of Augmentin from the APTES@Acid HNTs. Hence, the treated HNTs can be considered as a potential nanocarrier for effectively delivering Augmentin and promoting enhanced therapeutic benefits.

Preparation and characterization of quetiapine fumarate loaded transfersome as a novel drug delivery system

Modern medicine delivery techniques like transdermal patches are vital for treating numerous disorders. With the aid of TDDS, first pass metabolism is prevented, which aids in achieving effective bioavailability. Drug molecules are also released into the systemic circulation at a controlled and predetermined rate. The objective of this study was creating matrix-type Quetiapine fumarate loaded transdermal patches with water bath method using different polymers like HPMC 5 cps, HPMC 15 cps, and Ethyl cellulose in different ratios. Polyethylene glycol-400, Dimethyl sulfoxide (DMSO) as a plasticizer and permeation enhancer, Solvents including methanol and chloroform in 1:1 ratio employed. FT-IR study indicated that pure drug and excipients are compatible with each other. The formulated patches are evaluated for thickness, weight variation, folding endurance, percentage moisture content, percentage moisture uptake, drug content and In vitro diffusion studies. A transfersomal formulation containing 25 mg of the drug and 10 mg of span 80 was concluded as the optimized formulation (F1) as it showed maximum drug entrapment (84.8%) and cumulative percent drug release (98.51%)

Formulation and evaluation of preungual delivery system containing eugenol for the treatment of onychomycosis

The purpose of the study was to formulate a Preungual delivery system containing Eugenol for the treatment of Onychomycosis. And to find out the best polymer concentration, concentration of penetration enhancers and to carry out the anti-fungal testing on the best formulation obtained. The in vitro diffusion studies were carried out in Franz diffusion cell using phosphate buffer pH 7.4 and methanol as medium, whereas the permeation studies were carried out using hooves membrane. The percentage of cumulative drug released was determined by a UV spectrophotometer. The formulation containing 10% w/v of ethyl cellulose along with 2.5%w/v thioglycolic acid and 2.5 %v/v of dimethyl sulfoxide showed a good release. Eugenol nail lacquer's sensitivity against Candida albicans was determined by measuring the zone of inhibition by comparing it with a standard drug. The formulation showed a zero-order release pattern and the Higuchi model for the mechanism of release.

Formulation and Comprehensive Evaluation of Biohybrid Hydrogel Membranes Containing Doxycycline or Silver Nanoparticles.

Complicated wounds often require specialized medical treatments, and hydrogels have emerged as a popular choice for wound dressings in such cases due to their unique properties and the ability to incorporate and release therapeutic agents. Our focus was to develop and characterize a new optimized formula for biohybrid hydrogel membranes, which combine natural and synthetic polymers, bioactive natural compounds, like collagen and hyaluronic acid, and pharmacologically active substances (doxycycline or npAg). Dynamic (oscillatory) rheometry confirmed the strong gel-like properties of the obtained hydrogel membranes. Samples containing low-dose DOXY showed a swelling index of 285.68 ± 6.99%, a degradation rate of 71.6 ± 0.91% at 20 h, and achieved a cumulative drug release of approximately 90% at pH 7.4 and 80% at pH 8.3 within 12 h. The addition of npAg influenced the physical properties of the hydrogel membranes. Furthermore, the samples containing DOXY demonstrated exceptional antimicrobial efficacy against seven selected bacterial strains commonly associated with wound infections and complications. Biocompatibility assessments revealed that the samples exhibited over 80% cell viability. However, the addition of smaller-sized nanoparticles led to decreased cellular viability. The obtained biohybrid hydrogel membranes show favorable properties that render them suitable for application as wound dressings.

Fabrication and characterization of progesterone loaded pullulan nanofibers for controlled release

Progesterone is a commonly used drug in humans and livestock that possesses huge therapeutic potential in the regulation of pregnancy and fertility in females. The hydrophobicity and need for prolonged therapy of progesterone restrict the exploitation of its therapeutic potential to the fullest. Recently, polymeric nanofibers have evolved as interesting drug carriers, especially for hydrophobic drugs. The present study aimed to encapsulate the hydrophobic drug progesterone in pullulan by electrospinning for controlled delivery. The progesterone was successfully incorporated in pullulan nanofibers and the mean fiber diameter ranged from 68.68 ± 9.71 to 123.12 ± 17.41 nm. Fourier transform infrared spectroscopy revealed the interaction of the drug with the polymer. The zeta potential of progesterone loaded pullulan nanofibers ranged from 0.4 ± 0.01 to −0.5 ± 0.01 indicating suitability for transmucosal delivery. The hydrodynamic diameter of progesterone loaded pullulan nanofibers were significantly (p < 0.05) lesser than the pullulan nanofibers which may promote better drug adsorption and permeation. The cumulative drug release profile indicated prolonged release of progesterone for 7 days from pullulan nanofibers. The kinetic modelling of the drug release revealed Fickian diffusion of progesterone from the polymeric matrix. Cytotoxicity assay revealed optimal survivability of Baby Hamster Kidney cells (60.51 ± 5.81 to 72.39 ± 0.53 %) on exposure to progesterone loaded pullulan nanofibers ensuring biocompatibility. The present study presents process optimization for successful electro-entrapment of progesterone in biopolymer pullulan and its characterization suggesting the potential of progesterone loaded pullulan nanofibers for controlled delivery.

Metronidazole loaded chitosan–phytic acid polyelectrolyte complex nanoparticles as mucoadhesive vaginal delivery system for bacterial vaginosis

Bacterial vaginosis (BV) is a recurring infection that is difficult to treat due to the limited bioavailability of antimicrobials. In this study, Metronidazole (MTZ)-loaded chitosan nanoparticles (MCSNP) were synthesized employing phytic acid (PA) as a crosslinking agent for treating bacterial vaginosis. The prepared MCSNPs were characterized for size, shape, surface charge, compatibility, cytotoxicity, biofilm inhibition, and in-vitro/in-vivo antimicrobial activities. Morphological examination revealed that nanoparticles generated from 0.535 % w/v chitosan and 0.112 % w/v PA were non-spherical, discontinuous, and irregular, with zeta potential ranging from 25.00 ± 0.45 to 39 ± 0.7. The results of DSC and XRD demonstrated no change in the physical state of the drug in the finished formulation. The optimized formulation demonstrates a cumulative drug release of about 98 ± 1.5 % within 8 h. Antimicrobial studies demonstrated that the optimized formulation had enhanced efficacy against acid-adapted BV pathogens, with a MIC value of 0.9 ± 0.1 μg/mL. Compared to the MTZ alone, the in-vivo antibacterial results of in the case of developed nanoparticles showed a four-fold reduction in bacterial count in female Swiss albino mice. Based on the experimental findings, it was concluded that MCSNPs, due to their excellent physiochemical and antibacterial properties, could serve as a potential topical alternative for treating BV.

Temperature-Sensitive Aerogel Using Bagasse Carboxylated Cellulose Nanocrystals/N-Isopropyl Acrylamide for Controlled Release of Pesticides.

Temperature-sensitive carboxylated cellulose nanocrystals/N-isopropyl acrylamide aerogels (CCNC-NIPAMs) were developed as novel pesticide-controlled release formulas. Ammonium persulfate (APS) one-step oxidation was used to prepare bagasse-based CCNCs, and then the monomer N-isopropyl acrylamide (NIPAM) was successfully introduced and constructed into the temperature-sensitive CCNC-NIPAMs through polymerization. The results of the zeta potential measurement and Fourier infrared transform spectrum (FTIR) show that the average particle size of the CCNCs was 120.9 nm, the average surface potential of the CCNCs was -34.8 mV, and the crystallinity was 62.8%. The primary hydroxyl group on the surface of the CCNCs was replaced by the carboxyl group during oxidation. The morphology and structure of CCNC-NIPAMs were characterized via electron microscopy, X-ray diffraction (XRD), X-ray photoelectron spectroscopy (XPS), compression performance, porosity analysis, and thermogravimetric (TG) analysis. The results demonstrate that CCNC-NIPAM has a high porosity and low density, as well as good thermal stability, which is conducive to loading and releasing pesticides. In the swelling, drug loading, and controlled release process, the CCNC-NIPAM exhibited significant temperature sensitivity. Under the same NIPAM reaction amount, the equilibrium swelling rate of the CCNC-NIPAM first increased and then decreased with increasing temperature, and the cumulative drug release ratio of the CCNC-NIPAM at 39 °C was significantly higher than that at 25 °C. The loading efficiency of the CCNC-NIPAM on the model drug thiamethoxam (TXM) was up to 23 wt%, and the first-order model and Korsmyer-Peppas model could be well-fitted in the drug release curves. The study provides a new method for the effective utilization of biomass and pesticides.

Development of a new inhaled swellable microsphere system for the dual delivery of naringenin-loaded solid lipid nanoparticles and doxofylline for the treatment of asthma

This study developed a new dual delivery system of naringenin (NRG), a polyphenol, and doxofylline (DOX), a xanthine derivative, as an inhaled microsphere system. In this system, NRG has been first loaded into glyceryl tristearate-based solid lipid nanoparticles (NRG SLN), which were further loaded with DOX into swellable chitosan-tripolyphosphate-based microspheres (NRG SLN DOX sMS). The system was characterised based on particle size, PDI, zeta potential, surface morphology (SEM, AFM, and TEM), solid-state and chemical properties (XRD, IR, and NMR), aerodynamic parameters, drug loading, entrapment efficiency and in vitro drug release study. The optimised NRG SLN DOX sMS exhibited particle size, zeta potential, and PDI of 2.1 µm, 31.2 mV, and 0.310, respectively; a drug entrapment efficiency > 79%; a drug loading efficiency > 13%; cumulative drug releases of about 78% for DOX and 72% for NRG after 6 and 12 hours, respectively; good swelling and desirable aerodynamic properties. In addition, in vivo studies conducted in mice, a murine model of asthma showed significant reductions in serum bicarbonate and eosinophil counts and improvement in respiratory flow rate, tidal volume, and bronchial wall lining compared with the asthmatic control group. Overall, this novel inhalable dual-delivery system may represent a good alternative for the effective treatment of asthma.

Development and optimization of mouth-dissolving strips of L-methyl folate: A modern approach for patient compliance

The goal of this study is to create a mouth-melting strip of L-methyl folate calcium, which will dissolve and disintegrate more quickly when given orally for the onset of action. : Solvent casting was used to create a calcium L-methyl folate film that dissolves in the mouth. Polymer, plasticizer, and flavouring agents were chosen after early experiments. Once the excipients were chosen, 3 complete factorial designs were used to improve the formulation. Folding endurance (Y1), tensile strength (Y2), and disintegration time (Y3) were chosen as dependent variables, whereas HPMC E5 concentration (X1) and glycerine concentration (X2) were chosen as independent variables. The film's physicochemical parameters, including SEM, thickness, percent elongation, percent cumulative drug release, and palatability, were measured for the optimized batch and compared to those of the commercial product. The formulation of the mouth-dissolving strip took into account outcomes from the trial batch, including transparency, stickiness, and brittleness. The optimal batch has 55% HPMC E5 and 14.9% glycerine, with a folding endurance of 59±0.23, a tensile strength of 4.18±0.07 N/m, and a disintegration time of 40±0.12 seconds. The optimized film has dimensions of 0.08±0.01 mm in thickness, 60±1.58 mg in mass, 15.33±0.25% in elongation, and 98.33±0.27% in content uniformity. The SEM results validate the uniform film with uniform drug distribution. After 3 minutes, the L-methyl folate calcium mouth-dissolving strip had a %CDR of 99.42%. Findings of f2=52.85 and f1=12.5 for the similarity factor suggest that the medication release is clinically and commercially equivalent. One month of stability at 30°C and 65%RH was observed for the improved batch. The results of the created mouth-dissolving strip test are satisfactory, indicating the intended medication release. When compared to pills that dissolve in the mouth, it is clear that it is more patient-friendly.