Spontaneous Emulsification Method Research Articles

Formulation and characterization of nanoemulsion biopesticide from Balanite aegyptiaca seed kernel extract

Consumers’ growing awareness and desire for food free of pesticide residues led to the incubation of this research work. The study aimed at developing a nanoemulsion formulation of Balanite aegyptiaca seed kernel extract for use as a biopesticide. A preliminary study was carried out on the solubility and miscibility of surfactant, carrier, and deionized water utilizing the low-energy spontaneous emulsification method. Information from the study was then used to plot a ternary phase diagram (TPD) showing both the isotropic zone and the anisotropic zones, from which a point with a surfactant, oil, and water ratio (20:20:60) was selected from the isotropic zone for the formulation. The developed nanoemulsion was tested for stability and thermostability, and both results revealed the system was stable. Similarly, the physiochemical properties of the developed nanoemulsion system were characterized, and the results showed that the system revealed the following properties: mean particle size of 173.2±21.6, polydispersity index (PDI) of 0.403±0.038, surface tension of 32.53±0.71, viscosity of 37.33±0.67 mPas, and a pH of 4.92±0.02. The formulation appears homogeneous, clear, and transparent, which further indicates it’s a nanoemulsion formulation. Therefore, the nanoemulsion formulation of B. aegyptiaca seed kernel can serve as a safe and environmentally friendly substitute for synthetic pesticides in the management of plant diseases.

Fabrication and characterization of transdermal delivery of ribociclib nanoemulgel in breast cancer treatment

The objective of this study is to create a nanoemulgel formulation of Ribociclib (RIBO), a highly selective inhibitor of CDK4/6 through the utilization of spontaneous emulsification method. An experimental investigation was conducted to construct pseudo-ternary phase diagram for the most favourable formulation utilizing rice bran oil, which is known for its diverse anticancer properties. The formulation consisted of varying combination of the surfactant and as the co-surfactant (Tween 80 and Transcutol, respectively) referred to as Smix and the trials were optimized to get the desired outcome. The nanoemulsion (NE) formulations that were developed exhibited a droplet size of 179.39 nm, accompanied with a PDI of 0.211. According to the data released by Opt-RIBO-NE, it can be inferred that the Higuchi model had the most favourable fit among many kinetics models considered. The results indicate that the use of nanogel preparations for the topical delivery of RIBO in breast cancer therapy, specifically RIBO-NE-G, is viable. This is supported by the extended release of the RIBO, and the appropriate level of drug permeation observed in Opt-RIBO-NE-G. Due to RIBO and Rice Bran oil, RIBO-NE-G had greater antioxidant activity, indicating its effectiveness as antioxidants. The stability of the RIBO-NE-G was observed over a period of three months, indicating a favourable shelf life. Therefore, this study proposes the utilization of an optimized formulation of RIBO-NE-G may enhance the efficacy of anticancer treatment and mitigate the occurrence of systemic side effects in breast cancer patients, as compared to the use of suspension preparation of RIBO.

Antimicrobial and antioxidant competence of sustainable grumixama leaves extracts in nanoemulsion system

The spontaneous emulsification method was used to produce nanoemulsions loaded with grumixama leaves extracts (GLE) to protect and improve its functionality as a natural additive in food. Nanoemulsions were characterized for physicochemical stability, morphology, thermal analyses, antioxidant capacity, and antimicrobial activity. The formulations showed encapsulation efficiency (EE%) >89%, sizes between 182 and 290 nm, low polydispersity, and zeta potential near −30 mV. The formulations were kinetically stable since these parameters remained constant for up to 180 days at 4°C. The nanoemulsion with 125 mg GLE exhibited better droplet structure, which favored greater phenolic compounds protection and thermal resistance. The antioxidant capacity of all formulations remained stable over 30 days. The nanoemulsions acted as a bactericidal agent (MBC/MIC ratio ≤ 4) against Staphylococcus aureus, Bacillus cereus, and Listeria monocytogenes strains. However, GLE-loaded nanoemulsions offer a sustainable and functional alternative for use as a natural additive to meet trends such as a clean label.

Hesperidin nanoparticles for prostate cancer therapy: preparation, characterization and cytotoxic activity

Hesperidin, a phytochemical renowned for its therapeutic effects including anticancer, antioxidant, and anti-inflammatory properties, encounters a significant limitation in its application due to its low bioavailability and restricted solubility in water. To surmount these challenges, we employed a spontaneous emulsification method to produce hesperidin nanoparticles. These nanoparticles, averaging 197.2 ± 2.8 nm, exhibited uniform dispersion (polydispersity index: 0.13), a zeta potential (ZP) of −28 mV, encapsulation efficiency of 84.04 ± 1.3%, and demonstrated stable and controlled release across various environments. Assessment of the nanoemulsions stability revealed remarkably high stability levels. Cytotoxicity evaluations (3-(4,5-dimethylthiazol-2-yl)-2,5diphenyl-2-H-tetrazolium bromide, neutral red, trypan blue, and lactate dehydrogenase) indicated that cancer cell viability following treatment with hesperidin nanoemulsion was concentration and time-dependent, significantly lower compared to cells treated with free hesperidin. The colony formation assay and cell morphology evaluation further corroborated the heightened efficacy of hesperidin in its nano form compared to the free form. In summary, hesperidin nanoparticles not only exhibited more potent anticancer activity than free hesperidin but also demonstrated high biocompatibility with minimal cytotoxic effects on healthy cells. These findings underscore the potential for further exploration of hesperidin nanoparticles as an adjunctive therapy in prostate cancer therapy.

Fabrication of carotenoid enriched Crocus sativus w/o nanoemulsion: Optimization and pharmaceutical characterization

Herbal-based preparations have progressively attracted more interest nowadays due to multiple therapeutic approaches. Major concerns with the use of herbal preparations and their application as functional ingredients are about their stability, solubility, and bioaccessibility. Crocus sativus is one of the crucial nootropic traditional herbs, rich in potential phytochemicals used for the treatment of long-standing disorders. Many studies have suggested that the bioactive present in C. sativus extract may undergo enzymatic degradation in the intestine and hence less bioavailable at the site of action. A novel drug delivery approach to herbal preparation may combat the associated challenge. The present research focuses on the feasibility of developing w/o nanoemulsion incorporating the carotenoid-enriched C. sativus extract by spontaneous emulsification method. Critical process variables were optimized using 32 factorial design with Design of Expert software. The optimized formulation of w/o nanoemulsion comprising 9 mg/ml of C. sativus extracts with 12% internal phase, 21% S-mix, and 67% oil phase produced a globule size of 94.34 nm. The total content present in the nanoemulsion was 83% bioactive determined by the High Performance Liquid Chromatography- Photo Diode Array (HPLC-PDA) method. Further characterization, the Transmission Electron Microscopy (TEM) images showed the overall nanoemulsion system morphology with uniform distribution of globules of the internal phase. The in vitro release of bioactives from developed nanoemulsion showed an initial burst release of 60% at 1 hour following slow drug release. Results demonstrated that w/o nanoemulsion of C. sativus extract overcome the associated challenges and may reserve its space for medicinal application.

Formulation and Characterization of Glucosamine Sulphate Potassium Chloride (GSPC) Loaded Emulgel for the Treatment of Osteoarthritis.

Osteoarthritis (OA) is becoming a major medical burden worldwide due to changing lifestyles and aging populations. Osteoarthritis is a disease characterized by a variety of anatomic and physiological changes to joints, including cartilage degradation, bone remodeling, and the formation of osteophytes. These changes cause pain, stiffness, swelling, and limitations in joint function. Glucosamine serves as a fundamental constituent for cartilage, the resilient connective tissue responsible for cushioning joints. Glucosamine Sulphate Potassium Chloride (GSPC) supplementation is widely employed to mitigate symptoms linked to osteoarthritis, a degenerative joint disorder hallmarked by cartilage degradation. Palliative care aims at minimizing pain and disability and improving function, performance, and quality of life. In this study, the emulgel formulation of GSPC was developed and checked for its potential. Currently, OA does not have a definitive treatment. Since conventional dosage forms cannot deliver the active drug content at a predefined target site in a predictable manner throughout the treatment period, a new carrier system is always required. Considering their reduced size, targeting potential, and site specificity, nanocarrier-based approaches could hold an answer to shortcomings associated with conventional routes. Thus, the objective of the current study was to formulate and characterize glucosamine sulphate potassium chloride-loaded emulgel for the treatment of osteoarthritis. Microemulsion of glucosamine sulphate potassium chloride was formulated using a spontaneous emulsification method comprising of oleic acid (oil phase), Tween 80, Tween 20 (surfactant) and PEG 400, Span 80 (co-surfactant), and distilled water (aqueous phase). The microemulsions were evaluated for surface morphology, globule size, poly-dispersibility index (PDI), zeta potential, and viscosity, and the final batch of microemulsions was selected. The optimized microemulsion contained 35% co-surfactant (propylene glycol), 20% surfactant (Tween 20), and 15% oil (oleic acid) and glucosamine sulphate potassium chloride in a dose of 60 mg, which has sufficient drug loading capacity with a droplet size of 182 nm for optimized formulation. The optimized microemulsion formulation was added to gel prepared by Carbopol 934 in a 1:1 (w/w) ratio, leading to the formulation of glucosamine sulphate potassium chloride- containing emulgel. The prepared emulgel was further evaluated for viscosity, drug content, pH, and in-vitro drug release. Emulgel formulation (F6) showed 88% drug release after 6 hours, and it followed the Higuchi model. Glucosamine Sulphate Potassium Chloride (GSPC) is used in the treatment of OA by increasing the production of proteoglycans, which can cause the cartilage to break down. Emulgel formulation (F3) showed 75.41% drug release, and formulation (F6) showed 88% drug release after 6 h. Therefore, it may be concluded that an emulgel of GSPC can be used as a controlled-release dosage form of the drug for local application in OA.

Formulation and evaluation of fluconazole emulgels for potential treatment of vaginal candidiasis

Localised treatment of vaginal candidiasis could improve the therapeutic outcomes of patients with vaginal candidiasis as well as reduce drug dosage and dosing interval. The aim of the research project was to develop fluconazole emulgel formulations, and evaluate their physicochemical, drug release, antifungal, safety, and stability profile, for potential treatment of vaginal candidiasis. Xanthan gum and HPMC E5LV-based fluconazole emulgels were prepared using the spontaneous emulsification method and their physicochemical properties, drug content, drug release profile, anti-fungal activity against Candida albicans, in vivo vaginal biocompatibility and stability profile were evaluated using standard protocols. The fluconazole emulgels exhibited satisfactory properties: pH: 5.2–5.4; spreadability: 1.6–2.5 cm; apparent viscosity: 85–314 cP; zone of inhibition against Candida albicans: 22–38 mm; drug content: 91–102 %, and vaginal biocompatibility. All the studied fluconazole emulgels exhibited controlled fluconazole release over 6 h and their drug release kinetics fitted well with Korsmeyer-Peppas model. HPMC-based emulgels exhibited unsatisfactory real-time stability profile. To our knowledge, this is the first report where xanthan gum and HPMC E5LV-based fluconazole emulgels have been studied for possible treatment of vaginal candidiasis. Xanthan gum-based fluconazole emulgels are promising drug formulations that could reduce the drug dosage and dosing frequency. In addition, they could serve as alternative dosage forms to Flucos® gel.

Nanoemulsions and nanocapsules loaded with Melaleuca alternifolia essential oil for sepsis treatment.

Sepsis represents a complex clinical syndrome that results from a harmful host response to infection. The infections most associated with sepsis are pneumonia, intra-abdominal infection, and urinary tract infection. Tea tree oil (TTO) has shown high antibacterial activity; however, it exhibits low aqueous solubility and high volatility, which have motivated its nanoencapsulation. In this study, the performance of nanoemulsions (NE) and nanocapsules (NC) loaded with TTO was compared. These systems were prepared by spontaneous emulsification and nanoprecipitation methods, respectively. Poly-ε-caprolactone or Eudragit® RS100 were tested as polymers for NCs whereas Tween® 80 or Pluronic® F68 as surfactants in NE preparation. Pluronic® F68 and Eudragit® RS100 resulted in more homogeneous and stable nanoparticles. In accelerated stability studies at 4 and 25 °C, both colloidal suspensions (NC and NE) were kinetically stable. NCs showed to be more stable to photodegradation and less cytotoxic than NEs. After sepsis induction by the cecal ligation and puncture (CLP) model, both NE and NC reduced neutrophil infiltration into peritoneal lavage (PL) and kidneys. Moreover, the systems increased group thiols in the kidney and lung tissue and reduced bacterial growth in PL. Taken together, both systems showed to be effective against injury induced by sepsis; however, NCs should be prioritized due to advantages in terms of cytotoxicity and physicochemical stability.

EVALUATION OF CURCUMIN NANOEMULSION EFFECT TO PREVENT INTESTINAL DAMAGE

Curcumin has gained great prominence for the prevention and treatment of inflammatory bowel disease. However, studies have reported the low bioavailability of orally administered curcumin. This work aimed to evaluate the characteristics, stability and effects of a curcumin-carrying nanoemulsion in preventing intestinal damage induced by indomethacin. Nanoemulsions containing curcumin were prepared by spontaneous emulsification method and it was characterized by dynamic light scattering (DLS), zeta potential and the morphology was evaluated by scanning electron microscopy (SEM). Its stability was tested under different conditions of pH, temperature at 0, 7, 14, 21 and 28 days. In animal experimentation, 36 male mice of the Mus musculus lineage (C57BL/6) were used. The intestinal inflammation was evaluated based on macroscopic, histopathological and metagenomic analysis. It was found a stable nanoemulsion with a size of 409.8 nm, polydispersion index (PDI) of 0.132 and zeta potential of -18.8 mV. However, these lost charge in pH2, showing instability in acidic media (p< 0.05). In animal experiments, the nanoemulsion did not significantly improve intestinal inflammation. However, the group treated with curcumin nanoemulsion showed a higher relative abundance of the genus Lactobacillus (p<0.05). In conclusion, the curcumin nanoemulsion was relevant in the modulation of the intestinal microbiota.

Avaliação do uso de nanoemulsão de clorexidina a 0,25% na antissepsia da pele de gatos

ABSTRACT: This study evaluated the antiseptic effect of 0.25% chlorhexidine nanoemulsion (NM-Cl) on cat skin and compare its effect with that of 2.0% chlorhexidine digluconate (CS-Cl). NM-Cl was synthesized using the spontaneous emulsification method, and physical and chemical properties were analyzed. The antiseptic effects of NM-Cl and CS-Cl were randomly tested on the thoracic limbs of 10 healthy male cats. After a wide trichotomy of the thoracic limbs, NM-Cl was randomly applied to the trichotomy area of the right (n = 5) or left (n = 5) thoracic limbs. Then, a catheter was inserted aseptically in the cephalic vein. Subsequently, the same procedure was performed using CS-Cl on the contralateral limb. Cutaneous microbiota swab samples were obtained before antisepsis (Tpre); immediately after antisepsis (Tpost); and 4, 8, and 24 h after antisepsis. The collected samples were immediately inoculated on blood agar plates and incubated at 35 ºC ± 2 ºC in aerobiosis. Colony-forming units (CFUs) were manually counted after 24 h of inoculation. The Kruskal-Wallis and Mann-Whitney U tests were performed between groups and within the same group at different sample times, respectively. The NM-Cl and CS-Cl groups showed a reduction in CFUs between Tpre and Tpost in all animals (P &lt; 0.001). Both formulations presented an antiseptic effect 24 h of antisepsis (P &lt; 0.05), and no difference was observed between formulations at different times (P &lt; 0.05). With a lower concentration of chlorhexidine than CS-Cl, NM-Cl presents effective antiseptic action and prolonged residual effect in antisepsis for cat venipuncture.

Development, optimization, and characterization of rhein loaded nanoemulgel for treatment of osteoarthritis

This work aimed to design a transdermal delivery of rhein loaded nanoemulgel to improve the bioavailability and efficacy of rhein in the treatment of osteoarthritis and reduce its systemic side effects. Rhein loaded nanoemulsion (Rh-NE) prepared by application of ternary phase diagram and spontaneous emulsification method. Box-Behnken design (BBD) was employed to optimize formulation and preparation process of Rh-NE. The optimal formulation was 11.09% mixed oil (rhein and caproyl 90), 22.96% mixed emulsifier (kolliphor RH 40: transcutol HP, 1:1, w/w), and the preparation process was 23.08 min ultrasonic time and 179.5 W ultrasonic power. The particle size of the optimized Rh-NE was 24.5 ± 3.2 nm, PDI was 0.15 ± 0.02, and zeta potential was −18.6 ± 1.8 mV. The Rh-NE was incorporated into hydrogel consisted of 0.85% carbomer, 0.2% poloxamer 188 and 8.0% glycerol to form rhein loaded nanoemulgel (Rh-NE/Gel). In vitro transdermal flux of Rh-NE/Gel was 91.4 ± 0.9 μg/cm2·h. It was found that the inhibition rate of swelling degree of auricle caused by xylene was (54%), inhibition rate of writhing reaction was (60%), percentage increase in pain threshold was (P < 0.01), and the inhibition rate of capillary permeability was (69%). The therapeutic effect of Rh-NE/Gel on osteoarthritis in model rats was significantly improved compared with control group; the swelling degree of joint and toe were significantly reduced by 91% and 71%, respectively, and the contents of inflammatory factors IL-1β and NO were decreased 35.7% and 52.4%, respectively. The developed Rh-NE/Gel could provide anti-osteoarthritis effect and reduce the release of proinflammatory mediators in OA model rats.

Preparation of Idebenone as a Thermosetting Nasal Gel for Better Bioavailability and Histopathological Effect

Background Idebenone is an extensively metabolized drug with poor water solubility that is used to treat Leiber’s hereditary optical neuropathy. Objective This study aims to prepare idebenone nanoemulsion as a poloxamer-based nasal gel to overcome the extensive rate of hepatic metabolism for better bioavailability and lower histopathological effect on the nasal mucosa. Methods The formulation strategy was based on eliciting mutual concentration reduction between the nanoemulsion and the carrier gel by setting their gelation temperature between 30-32°C to overcome the mucociliary dose washout. The o/w nanoemulsions rely on cremophor EL and transcutol as an emulsifying system to stabilize idebenone-loaded lemongrass oil. The spontaneous emulsification method was used to prepare nanoemulsions that were characterized by zeta sizer while the thermosensitive hydrogels were prepared using the cold method. In-vitro dissolution test and ex-vivo permeation study through excised sheep nasal mucosa were performed to evaluate the enhanced permeation ratio, rate of permeation, and permeation coefficient. The histopathological effect of direct application on sheep nasal mucosa was studied using optical microscopy to evaluate cellular toxicity. Results The formula prepared from NE1 with poloxamer 407: poloxamer188 in concentrations 10:3% w/w respectively showed almost complete drug release in 120 minutes due to complete polymers blend erosion. Furthermore, thermosensitive nano-emulgel at a temperature of gelation 31.8°C was obtained at much lower concentrations of poloxamer 407 (10%) compared to previous studies. Nanoemulsions retained their globular size below 100nm due to further gel entrapment stabilization. Conclusions Drug permeation through excised sheep nasal mucosa elicited an increase in enhanced permeation ratio to 20.3 times and other flux kinetics parameters compared to those of IDB oil dispersion. Direct cellular toxicity showed a minor inflammatory response characterized by serous infiltration of inflammatory cells and edema. In contrast, most of the epithelial cells retained their histological characteristics compared to control slides. Received: Mar. 2023 Accepted: Aug 2023 Published: Oct.2023

Antibacterial food packaging capable of sustained and unidirectional release carvacrol/thymol nanoemulsions for pork preservation

Pork is highly susceptible to microbial spoilage and oxidative deterioration. In this work, an active packaging film capable of sustained and unidirectional release natural antimicrobials was developed to prolong the shelf life of chilled pork. Thymol&carvacrol nanoemulsions (TH&CA NEs) with two active constituents were prepared by low-energy spontaneous emulsification method and showed excellent antioxidant and antibacterial abilities. A trilayer film composed of loading, adhesive and barrier layers were fabricated using polyquaternium-10 (PQ-10)&carboxymethyl chitosan (CMC) microgels (denoted as PC), mixed solution of PQ-10 and zein (Z), and zein solution as raw material of each layer by layer-by-layer casting method. TH&CA@PC-PZ-Z packaging films were obtained by adding dropwise TH&CA NEs onto PC loading layer of PC-PZ-Z film and showed good interlaminar bonding strength, suitable water retention, satisfactory biological safety, as well as great antioxidant and antibacterial activities. In addition, most of TH&CA NEs in TH&CA@PC-PZ-Z films could be released from PC loading layer in a sustainable way for at least 7 days due to the block of Z barrier layer. The preservation effects of TH&CA@PC-PZ-Z films on chilled pork were further investigated in comparison with a plastic fresh-keeping film made by low-density polyethylene (LDPE). Results showed that TH&CA@PC-PZ-Z films could effectively retard lipid and protein oxidation and inhibit microbial growth during 11 days storage, thereby prolonged the shelf-life of chilled pork. We believe that the sustainable and unidirectional drug release film can be developed as a promising packaging film in preserving fresh meat products.

Nanoemulsions as medicinal components in insoluble medicines

Background: Medicine’s success relies on solubility, which is the process of dissolving a solid substance in a fluid phase to create a uniform molecular dispersion. However, hydrophobic active medicinal components exhibit poor solubility in water, limiting their effectiveness and incorporation into medications. Aim: This review explores the potential of nanoemulsions as a solution for delivering hydrophobic medicinal components with low solubility. The study investigates the benefits of nanoemulsions, including enhanced absorption, effective targeting, controlled release, and protection of encapsulated bioactive ingredients. Materials and methods: Nanoemulsions are formulated by combining two immiscible liquids with emulsifying agents within a thermodynamically stable colloidal dispersion system. The review categorizes various preparation techniques into high-energy and low-energy spontaneous emulsification methods. The choice of preparation procedures and materials used significantly affects the stability of nanoemulsions over time. Evaluation of nanoemulsions includes studying medication release in vitro, in vitro permeation, stability and thermodynamic stability, shelf life, viscosity, interfacial tension, pH, and osmolarity. Results: Nanoemulsions, such as Celecoxib (Phase Inversion), acetylsalicylic acid (Ultrasonication), and Flurbiprofen (Homogenization and Ultrasonication), offer distinct advantages for medications with low solubility compared to conventional emulsions. These nanoemulsions comprise small droplets with a larger surface area, promoting enhanced absorption. They demonstrate effective targeting, controlled release, and protection of encapsulated bioactive ingredients. Moreover, the diminutive droplet sizes of nanoemulsions contribute to their reduced susceptibility to issues like flocculation, coalescence, sedimentation, or creaming. Conclusion: Nanoemulsions hold great promise in overcoming the solubility limitations of hydrophobic medicinal components. They provide enhanced absorption, effective targeting, controlled release, and protection of bioactive ingredients. The choice of preparation techniques and materials plays a crucial role in ensuring the stability of nanoemulsions over time. Further studies are warranted to optimize their use and explore their potential applications in drug delivery systems.

THE INFLUENCE OF CATHARANTHUS ROSEUS (L.) G. DON. ETHANOL EXTRACT IN CLOVE OIL NANOEMULSION: PHYSICAL CHARACTERIZATION, ANTIOXIDANT AND ANTIBACTERIAL ACTIVITIES

Objective: This study aimed to develop a topical nanoemulsion using clove oil and ethanol extract of catharanthus roseus (L.) G. for antioxidant and antibacterial dosage form. Methods: The nanoemulsion was produced using a spontaneous emulsification method. The formulation was carried out using tween 80 and pluronic 127 as surfactants with different extract concentrations (0.5–2%). The characterizations of the formula included organoleptic test, homogeneity, pH determination, emulsion type, viscosity, particle size determination, zeta potential, and stability test were evaluated. Antioxidant activity was conducted using DPPH method and antibacterial activity was determined against propionibacterium acnes and Staphylococcus epidermidis. Results: The result showed that all the formulations produced a stable nanoemulsion with semisolid, clarity, transparent and homogenous characteristic. The nanoemulsion had pH of 5.5-6.5 and belong to oil in water (O/W) type of emulsion. The formula showed viscosity ranged from 121.33±0.29 until 211.01±1.00 cps, had particle size below than 300 nm, and were stable for 3 mo of storage and after accelerated evaluation. nanoemulsion contained 2% of c. roseus extract showed moderate antioxidant activity with IC50 value of 96.29±3.64 and antibacterial activity with 10.65±0.15 and 13.27±0.21 mm of inhibition zones for propionibacterium acnes and Staphylococcus epidermidis, respectively. Conclusion: Clove oil combined with the ethanol extract of c. roseus produced a stable nanoemulsion, which demonstrated concentration-dependent antioxidant and antibacterial activities.

Antimicrobial Photodynamic Therapy against Escherichia coli and Staphylococcus aureus Using Nanoemulsion-Encapsulated Zinc Phthalocyanine.

Multidrug-resistant microorganisms have become a significant public health threat, and traditional antibiotics are becoming ineffective. Photodynamic therapy (PDT) is a promising alternative that utilizes photosensitizers and light to produce Reactive Oxygen Species (ROS) that can kill microorganisms. Zinc phthalocyanine (ZnPc) is a promising photosensitizer due to its strong affinity for encapsulation in nanoemulsions and its antimicrobial properties. In this study, nanoemulsion was prepared using Miglyol 812N, a surfactant, and distilled water to dissolve hydrophobic drugs such as ZnPc. The nanoemulsion was characterized by its particle size, polydispersity index, Transmission Electron Microscope and Zeta potential, and the results showed that it was an efficient nanocarrier system that facilitated the solubilization of hydrophobic drugs in water. The use of ZnPc encapsulated in the nanoemulsion produced through the spontaneous emulsification method resulted in a significant reduction in cell survival percentages of gram-positive Staphylococcus aureus and gram-negative Escherichia coli by 85% and 75%, respectively. This may be attributed to the more complex cell membrane structure of E. coli compared to S. aureus. This demonstrates the potential of nanoemulsion-based PDT as an effective alternative to traditional antibiotics for treating multidrug-resistant microorganisms.

Fabrication of poloxamer based besifloxacin thermosensitive in situ gelling nanoemulsions for ophthalmic delivery

The present study aimed to develop and investigate besifloxacin (BSF) in situ gel nanoemulsions (NEs) consisting of two hydrophilic polymers, that is, poloxamer 407 (P407) and poloxamer 188 (P188), for ocular delivery. BSF loaded in situ gel-NEs containing triacetin (oil), Cremophor®RH 40 (surfactant), Transcutol®P (co-surfactant), poloxamer 407 and poloxamer 188 (gelling agents) were prepared by spontaneous emulsification method. The optimum in situ gel nanoemulsion was selected based on gelation temperature. The selected formulation was evaluated for physicochemical characteristics, including droplet size, refractive index, pH, transparency, and viscosity. Further investigations such as in vitro drug release, ex vivo corneal permeation, HET-CAM, pre-corneal residence time antibacterial efficacy studies were conducted too. Developed BSF in situ gel nanoemulsion showed acceptable physicochemical properties with a nano-metric droplet size of 19 nm and PDI of 0.21. Moreover, In vitro release studies revealed that the in situ gel formulation could sustain drug release as only 40% of the BSF was released within 1 h. Permeability coefficient (Papp) of BSF through the excised bovine cornea was found 6.01 × 10−6 cm/s during 6 h. In addition, the HET-CAM evaluation confirmed the non-irritancy of the optimum BSF in situ gel NEs. The pre-corneal residence time evaluation indicated prolonged retention of in situ gel-NEs on the eye surface. Finally, antibacterial susceptibility investigations illustrated remarkable efficacy against Pseudomonas aeruginosa and Staphylococcus aureus. The current findings demonstrated that this proposed BSF-loaded in situ gel-NEs could be considered as a potential novel drug delivery formulation against ophthalmic bacterial infections.

Metastatic Melanoma: A Preclinical Model Standardization and Development of a Chitosan-Coated Nanoemulsion Containing Temozolomide to Treat Brain Metastasis.

Melanoma is the most aggressive type of skin cancer. Brain metastasis is the worst scenario in metastatic melanoma and the treatment options for these patients are limited. Temozolomide (TMZ) is a chemotherapy agent used to treat primary central nervous system tumors. Our objective was to develop chitosan-coated nanoemulsion containing temozolomide (CNE-TMZ) for nasal route administration to melanoma brain metastasis treatment. A preclinical model of metastatic brain melanoma was standardized, and the efficiency of the developed formulation was further determined in vitro and in vivo. The nanoemulsion was done by spontaneous emulsification method and the formulation was characterized by size, pH, polydispersity index, and zeta potential. Culture assessments to determine cell viability were done in the A375 human melanoma cell line. To determine the safety of formulation, healthy C57/BL6 mice were treated with a nanoemulsion without TMZ. The model in vivo used B16-F10 cells implanted by stereotaxic surgery in C57/BL6 mice brains. The results demonstrate that the preclinical model used showed to be useful to analyze the efficiency of new candidate drugs to treat melanoma brain metastasis. The chitosan-coated nanoemulsions with TMZ showed the expected physicochemical characteristics and demonstrated safety and efficacy, reducing around 70% the tumor size compared to control mice, and presenting a tendency in mitotic index reduction, becoming an interesting approach to treat melanoma brain metastasis.

Fabrication, characterization, antimicrobial, toxicity and potential drug-delivery studies of PEGylated Sesamum indicum oil based nanoemulsion system

BackgroundThe actively mutating properties of disease-causing pathogens and GI intolerance associated with certain antibiotics among other challenges necessitated the adoption of colloidal system for drug delivery. Nanoemulsions (Ciprofloxacin (Cp) -loaded and non-drug loaded) were prepared by spontaneous emulsification method, characterized using Cryo-TEM, FTIR and Zetasizer. Antimicrobial activities were carried out using agar well diffusion method on Klebsiella pneumoniae and Bacillus subtilis. The in-vitro and dermal toxicological assessment were carried out using adult Wistar rats.ResultsThe Cryo-TEM micrographs showed spherical morphology while zetasizer results showed polydispersity index (PDI), mean droplet size and zeta potential (ZP) of 0.553, 124.3 ± 0.29 nm and − 15.3 mV respectively for non-drug loaded sesame oil-based emulsion (SOAB). While 0.295, 244.8 ± 0.33 nm and − 5.54 mV were recorded for Cp-loaded sesame oil-based emulsion (SOAB + Cp). The effective voltage charge of the emulsions was 147.4 V. FTIR results of Cp recorded O–H adsorption value of 3429 cm−1, while SOAB and SOAB + Cp showed superimposition at 3427.76 cm−1 showing no drug-excipient interactions. No skin irritation was observed after 14 days of skin corrosion assessment. No significant difference (p > 0.05) in body weight gain of both test and control animals, the treatment did not cause any observable alterations in blood-chemistry parameters and hematological indices. Photomicrographs of liver and heart shows an uncompromised histological architecture.ConclusionThe finding of the study shows a skin friendly, nanosized, spherical negatively charged emulsion with no cardiotoxic, hematotoxic and hepatotoxic effects on Wistar rats, and as such appears promising as a safe vehicle for drug delivery.Graphical

Polymeric encapsulation of anti-larval essential oil nanoemulsion for controlled release of bioactive compounds

In the present study, polymeric encapsulation of lemongrass oil nanoemulsion was done for the controlled release of bioactive compounds. O/W nanoemulsion was prepared from lemongrass essential oil, non-ionic surfactant polysorbate80 and water by spontaneous emulsification method. Geranial and neral were found to be the major bioactive compounds, constituting 45.1 % and 31.1 % of total lemongrass essential oil. The optimized lemongrass oil nanoemulsion was formulated with the droplet diameter of 14.4 nm and polydispersity index of 0.111. Transmission electron micrographs revealed that the nanoemulsion droplets were spherical in morphology and were in the size range of 10–100 nm. The optimized nanoemulsion was encapsulated with chitosan polymer by using glutaraldehyde as a cross-linking agent. Encapsulation of essential oil nanoemulsion was optimized for the process parameters such as chitosan concentration and nanoemulsion concentration in order to obtain applicable encapsulation with enhanced release of lemongrass oil. The essential oil-loaded microcapsules were spherical and smooth in shape as revealed by phase contrast microscopy and scanning electron microscopy (SEM) with the diameter of 0.53 ± 0.02 mm. Mosquito larvicidal activity of encapsulated essential oil nanoemulsion was better against malaria vectors Anopheles stephensi and Anopheles culicifacies when compared to non-encapsulated nanoemulsion, due to the controlled release of the bioactive components. The results of this study will be helpful for future vector control strategies as we provided a practical combined technique of nanoemulsion formulation and polymeric encapsulation as potential delivery system of hydrophobic bioactive compounds against mosquito vector.