Nanoemulsifying Drug Delivery System Research Articles

Evaluation of oral bioavailability and other pharmacy effects on sleep quality by using zaleplon nano emulsifying drug delivery systems carrying

Evaluation of oral bioavailability and other pharmacy effects on sleep quality by using zaleplon nano emulsifying drug delivery systems carrying

Curcumin Administration Routes in Breast Cancer Treatment.

Breast cancer is a public health concern worldwide, characterized by increasing incidence and mortality rates, requiring novel and effective therapeutic strategies. Curcumin is a bioactive compound extracted from turmeric with several pharmacological activities. Curcumin is a multifaceted anticancer agent through mechanisms including the modulation of signaling pathways, inhibition of cell proliferation, induction of apoptosis, and production of reactive oxygen species. However, the poor water solubility and bioavailability of curcumin create important barriers in its clinical application. This review elaborates on the therapeutic potential of curcumin in breast cancer treatment, focusing on the efficacy of different administration routes and synergistic effects with other therapeutic agents. The intravenous administration of curcumin-loaded nanoparticles significantly improves bioavailability and therapeutic outcomes compared to oral routes. Innovative formulations, such as nano-emulsifying drug delivery systems, have shown promise in enhancing oral bioavailability. While intravenous delivery ensures higher bioavailability and direct action on tumor cells, it is more invasive and expensive than oral administration. Advancing research on curcumin in breast cancer treatment is essential for improving therapeutic outcomes and enhancing the quality of life of patients.

Demystifying the Potential of Embelin-Loaded Nanoformulations: a Comprehensive Review.

Phytoconstituent based therapies have the potential to reduce the adverse effects and enhance overall patient compliance for different diseased conditions. Embelin (EMB) is a natural compound extracted from Embelia ribes that has demonstrated high therapeutic potential, particularly as anti-inflammatory and anticancer therapeutic applications. However, its poor water solubility and low oral bioavailability limitations make it challenging to use in biomedical applications. Nanostructure-based novel formulations have shown the potential to improve physicochemical and biological characteristics of active pharmaceutical ingredients obtained from plants. Different nanoformulations that have been utilized to encapsulate/entrap EMB for various therapeutic applications are nanoliposomes, nanostructured lipid carriers, niosomes, polymeric nanoparticles, nanosuspensions, phytosomes, self nanoemulsifying drug delivery system, silver nanoparticles, microparticles, solid lipid nanoparticle, gold nanoparticles and nanomicelles. The common methods reported for the preparation of EMB nanoformulations are thin film hydration, nanoprecipitation, ethanol injection, emulsification followed by sonication. The size of nanoformulations ranged in between 50 and 345nm. In this review, the mentioned EMB loaded nanocarriers are methodically discussed for size, shape, drug entrapment, zeta potential, in vitro release & permeation and in vivo studies. Potential of EMB with other drugs (dual drug approach) incorporated in nanocarriers are also discussed (physicochemical and preclinical characteristics). Patents related to EMB nanoformulations are also presented which showed the clinical translation of this bioactive for future utilization in different indications.

Optimization and Characterization of Self Nano Emulsifying Drug Delivery System (SNEDDS) Naringenin Components with D-Optimal Mixture Design Method and Anti-Aging Test In Vivo

Optimization and Characterization of Self Nano Emulsifying Drug Delivery System (SNEDDS) Naringenin Components with D-Optimal Mixture Design Method and Anti-Aging Test In Vivo

Solid Self Nano-Emulsifying Drug Delivery System of Dasatinib: Optimization, In-vitro, Ex-vivo and In-vivo assessment.

Aim: Dasatinib (DST) is an oral tyrosine kinase inhibitor with poor aqueous solubility. To outwit this issue, a solid self-nano emulsifying drug delivery system (S-SNEDDS) of DST was formulated.Methods: I-optimal mixture design was used for optimization of DST-loaded SNEDDS using Linalool, Cremophor RH40 and Transcutol P. S-SNEDDS underwent physicochemical characterization, in-vitro release and ex-vivo permeation, cell-based assays and pharmacokinetic study.Results: DST-S-SNEDDS showed globule size and PDI of 141.53±5.371nm and 0.282±0.020, respectively. DST-S-SNEDDS revealed significantly lower IC50 (1.825μg/mL) than free DST (7.298μg/mL) in MDA-MB-231. In-vivo pharmacokinetic study revealed 1.94-fold increment in AUC0-t for the DST-S-SNEDDS group than free DST.Conclusion: S-SNEDDS could be promising approach for improving bioavailability and efficacy of DST.

The Abundance of Bioactive Compounds in Fingerroot Essential Oil Before and After Self Nanoemulsifying Drug Delivery System (SNEDDS) as a Potential Substitute for Synthetic Antibiotics in Livestock

The Abundance of Bioactive Compounds in Fingerroot Essential Oil Before and After Self Nanoemulsifying Drug Delivery System (SNEDDS) as a Potential Substitute for Synthetic Antibiotics in Livestock

D-Optimal Mixture Design Enabled Development of Lyophilized Nanoemulsifying Drug Delivery System of Paliperidone

Background: Schizophrenia is a chronic disease with acute psychotic symptoms, which is having frequent recurrence. Paliperidone palmitate (PP) is a second-generation antipsy-chotic drug to treat schizophrenia. Aims: The aim of the study was to prepare lyophilized nanoemulsifying drug delivery system (NEDDS) of paliperidone (PD). Objective: The primary objective of the current research work was to develop a lyophilized nanoemulsifying drug delivery system (NEDDS) of paliperidone (PD) to improve its oral bioa-vailability and stability. Methods: Optimization using D-Optimal Mixture Design DMD) was conducted, and optimized NEDDS was further lyophilized to improve stability. The lyophilized optimized NEDDS was fur-ther evaluated for biopharmaceutical evaluation. Result: A saturation solubility study revealed Peceol, Tween 80, and Plurol Olique CC497 as suitable candidates for oil, surfactant, and co-surfactant, respectively. Optimized NEDDS of PD showed mean globule size (MGS) of 185 nm, PDI of 0.27 and cumulative % drug release within 15 min Q15 of 86.6%. Lyophilized optimized NEDDS was found to have no significant change in quality attributes within the stability study period. A pharmacokinetic study revealed more than two-fold increases in bioavailability for lyophilized optimized NEDDS. Conclusion: Hence, lyophilized NEDDS of PD can be used as an effective approach for the im-provement of oral bioavailability and stability.

Dissolution and antioxidant potential of apigenin self nanoemulsifying drug delivery system (SNEDDS) for oral delivery

Self-nanoemulsifying drug delivery systems (SNEDDS) have been used to improve the oral bioavailability of various drugs. In the current study, apigenin was developed as SNEDDS to solve its dissolution problem and enhance oral bioavailability and antioxidant potential. SNEDDS were prepared by mixing Gelucire 44/14, Tween 80, and PEG 400 under controlled conditions. The droplet of diluted SNEDDS demonstrated a spherical shape with a size of less than 100 nm and a neutral charge. The very fast self-emulsification was obtained within 32 s, and the transmittance values exceeded 99%. The highest drug loading was 90.10 ± 0.24% of the initial load with the highest %encapsulation efficiency of 84.20 ± 0.03%. FT-IR and DSC spectra showed no interaction between components. The dissolution in buffer pH 1.2, 4.5, and 6.8 showed significantly higher dissolved apigenin than the apigenin coarse powder. The dissolution profiles were fitted to the Korsmeyer–Peppas kinetics. The cellular antioxidant activities in Caco-2 cells were approximately 52.25–54.64% compared to no treatment and were higher than the apigenin coarse powder (12.70%). Our work highlights the potential of SNEDDS to enhance the dissolution and permeability of apigenin and promote antioxidant efficacy, which has a strong chance of being developed as a bioactive compound for nutraceuticals.

Enhancing the Antiproliferative Activity of Perillyl Alcohol against Glioblastoma Cell Lines through Synergistic Formulation with Natural Oils.

Due to its volatility, photostability, and gastrointestinal toxicity, Perillyl Alcohol (POH), a monoterpenoid component of various plant species, is a chemotherapeutic drug with insufficient efficacy. Many naturally occurring bioactive compounds have well-known antiproliferative properties, including sefsol, jojoba, tea tree, and moringa oils. This study sought to develop an oil-based Self Nanoemulsifying Drug Delivery System (SNEDDS) using tween 80 as the surfactant and Dimethyl Sulfoxide (DMSO) or Polyethylene Glycol (PEG) 400 as the cosurfactant; the oils were used in a range of 10-20% to boost POH's anticancer efficacy. The formulations' size, charge, and impact on the viability of glioma cell lines, ANGM-CSS and A172, were evaluated. The developed SNEDDS formulations ranged from 3 nm to 362 nm in size, with electronegative surface charges between 5.05 and 17.0 mV and polydispersity indices between 0.3 and 1.0. The findings indicated that the antiproliferative effect of POH-loaded Nanoemulsion (NE) could be used as a possible anticancer therapy for glioblastoma in vitro, particularly when paired with the tested natural oils. Before asserting that this delivery technique is appropriate for glioblastoma therapy, additional in vitro and in vivo investigations are required.

An Overview of Self Nano-emulsifying Drug Delivery Systems for Enhanced Solubility and Dissolution for Anti-cancer Drugs

The current review aims to explore recently identified chemical compounds, particularly focusing on the challenge posed by the poor water solubility of many existing drug molecules. This limitation significantly affects the successful development and marketability of new pharmaceuticals, as the dissolution phase often becomes the bottleneck in the process. Crafting formulations becomes crucial in enhancing the absorption and, consequently, the oral effectiveness of these drug prospects. Given the prevalence of various diseases such as cancer, AIDS, HIV, and chronic inflammation among humans, optimizing drug delivery methods becomes pivotal to achieving maximum therapeutic benefits with minimal side effects. Innovative drug delivery systems like self-nano-emulsion are introduced, offering protective measures for medications, augmenting their characteristics, and elevating solubility and bioavailability. Furthermore, this study aims to enhance the chemical and physical stability of these compounds during extended periods of storage. Ultimately, this research endeavours to provide insights into the efficacy of self-nano-emulsion in enhancing solubility and bioavailability, thereby aiding researchers in comprehending its potential applications.

Design Expert-Implemented Nimodipine-Loaded Lyophilized Nanoemulsifying Drug Delivery System for Improved Oral Bioavailability and Physical Stability

Design Expert-Implemented Nimodipine-Loaded Lyophilized Nanoemulsifying Drug Delivery System for Improved Oral Bioavailability and Physical Stability

Self Nanoemulsifying Drug Delivery System: A Comrhensive Review

SNEDDS is also important to create a wide interface for distributing the hydrophobic drug between the oil and aqueous phase, increasing the overall bioavailability of the drug.This process can be stabilized using emulsifiers that reduce interfacial tension.Self-nanoemulsified dosage forms can improve the oral bioavailability of biopharmaceutical class II and IV drugs, The potential mechanism by which SNEDDS increases oral bioavailability.Oral administration of peptides due to proteins is a very difficult task due to poor water quality, poor permeability and tolerance of intestinal environmental stability. Many strategies are being investigated to increase the oral absorption of protein. Recently, evaluated the ability of SNEDDS to improve the oral bioavailability of β-lactamase, a model protein. SNEDDS to the solid state can reduce chemical degradation, but in many cases does not eliminate it. Therefore, it is important to identify microenvironment modification strategies to improve the stability of pH-sensitive drugs.

Triamcinolone-loaded self nano-emulsifying drug delivery systems for ocular use: An alternative to invasive ocular surgeries and injections

Inflammation of the posterior segment of the eye is a severe condition and hard to cure as delivery of drugs to the inflammation site is inefficient. Currently, the primary treatment approach is ocular surgery or invasive ocular injections. Herein, we designed and developed a topically self nano-emulsifying drug delivery system (SNEDDs) to deliver triamcinolone acetonide (TCA) to the posterior segment of the eye. A screening based on TCA solubility was conducted on each excipient followed by preparation of various formulations using different ratios of the selected excipients. Vesicles of optimized SNEDDs had less than 100 nm size and spherical morphology. 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay showed self-emulsified vesicles have relatively high safety on retinal pigment epithelium (RPE) cell line. Furthermore, efficient cellular uptake of coumarin 6-loaded SNEDDs in RPE using confocal laser scanning microscopy (CLSM) was confirmed.In addition, an in-vivo study using hematoxylin and eosin (H&E) staining revealed that 14 days of topical treatment of albino rabbit eyes with TCA-loaded SNEDDs was safe and no sign of tissue destruction and inflammation was detected in different parts of the eye sections including cornea, sclera, retina, and optic nerve. Also, the CLSM images from topically treated eyes with coumarin 6 (a hydrophobic, fluorescent drug model) loaded SNEDDs, showed that the optimized SNEDDs could properly penetrate toward the posterior segments of the eye especially the retina, posterior parts of the choroid, and sclera. Considering the outstanding results obtained by ocular tissue penetration and low toxicity, prepared SNEDDs, have the potential to be used as a topical administration for treating posterior segment disorders of the eye through an utterly non-invasive route and TCA-loaded SNEDDs could be an alternative for TCA intravitreal and intra conjunctival injections.

Evaluation of Stability and In vitro Anti-Cancer Activity of Dihydroquercetin Nanoemulsion

Background: Dihydroquercetin (DHQ), also known as taxifolin, is a flavonoid commonly found in many plants. Dihydroquercetin has been documented to have powerful antioxidant activity and many beneficial properties for human health, especially its ability to inhibit certain types of cancer cells. However, its low solubility and bioavailability are major obstacles to biomedical applications. Moreover, DHQ is chemically unstable and quickly degrades when exposed to alkaline conditions. background: Dihydroquercetin (DHQ), also known as taxifolin, is a flavonoid and commonly found in many plants. Dihydroquercetin has been documented to have powerful antioxidant activity and many beneficial properties for human health, especially its ability to inhibit certain types of cancer cells. However, its low solubility and bioavailability are major obstacles to biomedical applications. Moreover, DHQ is chemically unstable and quickly degrades when exposed to alkaline conditions. Objective: In the present study, a DHQ nanoemulsion formulation was prepared by Self Nano- Emulsifying Drug Delivery System (SNEDDS) technique to overcome the above disadvantages. Methods: The obtained nanoemulsion system was evaluated for its micro-properties, stability, and in vitro cytotoxic activity against some cancer cells using tetrazolium dyes (MTS assay). Results: Measurement results showed that the DHQ nanoemulsion was successfully synthesized with typical mean droplet sizes from 9 to 11 nm, and revealed excellent stability over time. Dihydroquercetin in nanoemulsion form is more stable than the non-encapsulated form, as evidenced by the maintenance of droplet size in the nanometer range when dispersed in aqueous solution for up to 48 hours. This stability is particularly pronounced in both acidic and neutral environments. In vitro experiments on cytotoxic activities against A549, Hela, and HepG2 cancer cell lines indicated that the prepared DHQ nanoemulsion effectively inhibited the growth of all these cell lines with IC50 values (μg/mL) of 8.0, 20.4, and 29.5 respectively. Conclusion: From the detailed results above, it is evident that the solubility and bioavailability of DHQ can be improved by creating its nanostructure in the form of nanoemulsions. Furthermore, the nano form of DHQ carried within stable nanoemulsions exhibited better performance in inhibiting cancer cells compared to free DHQ. Therefore, further research is required to explore the development of cancer therapeutics utilizing nano DHQ emulsions.

Formulation and Characterization of Mefenamic Acid Self Nanoemulsifying Drug Delivery System (SNEDDS) Preparations

Mefenamic acid is included in BCS (biopharmaceutical classification system) class II, namely high permeability and low solubility. This research aims to obtain a good formula for oleic acid oil, tween 80, and PEG 400 according to the characterization test of emulsification time, % transmittance, drug loading, globule size, and zeta potential. This research was an experimental study by formulating mefenamic acid in the form of SNEDDS which was made 1 formula was made in the form of SNEDDS with the composition of oleic acid, tween 80, and PEG 400 and characterization tests were carried out for emulsification time, % transmittance, drug loading, globule size, zeta potential. The yield of the oleic acid formula is 1%, tween 80 is 8%, and PEG 400 is 1%. The emulsification time characterization test resulted in 17 seconds, % transmittance of 97%, drug loading of 179.81 mg, globular size of 85.8 nm and zeta potential of -1.6 mV.

Enhancement of lcariin aphrodisiac effect by self nano emulsifying drug delivery system (SNEDDS) method ‎

Enhancement of lcariin aphrodisiac effect by self nano emulsifying drug delivery system (SNEDDS) method ‎

Nanoemulsion drug delivery system loaded with imiquimod: a QbD-based strategy for augmenting anti-cancer effects

BackgroundSkin cancer is becoming a public health concern due to increased exposure to environmental pollutants and UV rays, among other factors. In India, skin neoplasms constitute 2–3% of all human cancer cases, whereas in the USA, 2–3 million cases of non-melanoma skin cancer are reported annually. Various drugs are available in the market for treating skin cancer. Imiquimod (IMQ) is one such drug approved by the USFDA for managing basal cell malignancy, external genital warts, and actinic keratosis. The conventional dosage form of IMQ cream has several side effects that can lead to therapy interruption. Therefore, the present work aims to develop an IMQ nanoemulsion with improved solubility, in vitro drug release and stability. Nanoemulsion was formulated using oleic acid/rose oil, with polysorbate 20/propylene glycol selected as the oil phase and Smix, respectively. Optimization carried out using a 32 factorial design with the aid of a quadratic model. Characterization was conducted for parameters, namely viscosity, pH, drug content, globule size, zeta potential and entrapment efficiency. Thermodynamic stability studies were conducted to assess the stability of the formulation. Furthermore, the optimized system was subjected to TEM analysis, in vitro drug release and in vitro cytotoxicity assay (MTT assay).ResultsNanoemulsions were found to be in the size range of 152.80–470.13 nm and exhibited a spherical shape. Zeta potential values ranged from − 28.93 to − 58.48 mV. DSC measurements indicated the complete solubilization of IMQ in the nanoemulsion system. The optimized formulation F1 displayed the following characteristics: a globule size < 200 nm, a zeta potential > − 55 mV, a polydispersity index < 0.2, % drug content of 102.89 ± 1.06, % entrapment efficiency of 97.59 ± 0.24, a pH of 4.77 ± 0.06, and a viscosity of 4.06 ± 0.06 poise. In vitro IMQ release studies of nanoemulsion and commercial cream showed approximately 70% and 34% drug release, respectively, at the end of 8 h. Moreover, the in vitro cytotoxicity assay depicted that F1 exhibited greater cytotoxic potential compared to the commercial formulation against the A431 cell line.ConclusionThe present investigation showed a significant improvement in in vitro drug release of the BCS class IV drug IMQ and enhanced cytotoxic activity against cancerous cells. IMQ-loaded nanoemulsion represents a promising vehicle for delivering treatment to the skin for treating skin cancer.Graphical abstract

Preparation of oral nanoemulsion drug delivery system loaded with punicalagin: in vitro antibacterial activity, drug release, and cell safety studies

Preparation of oral nanoemulsion drug delivery system loaded with punicalagin: in vitro antibacterial activity, drug release, and cell safety studies

Itraconazole Self-Nano Emusifying Drug Delivery System for Enhancement of Solubility

The main objective of formulation is to enhance the bioavailability of the drug within the body. Some of the challenging subjects associated with poorly water-soluble drugs concern solubility and bioavailability factors. To overcome these problems, new technologies, such as lipid-based drug delivery systems including micro or nano emulsifying drug delivery system, have obtained importance in recent years, due to their enhanced solubility and bioavailability in the gastrointestinal tract. Such systems are solubilized within the lipid excipients or mixed with oils or surfactants/co-solvents to facilitate the solubility and absorption rate, which can enhance the bioavailability of the targeted drug. The research was targeted to develop a self-Nano Emulsifying drug delivery system (SNEDDS) for oral bioavailability enhancement of BCS II antifungal drug Itraconazole. Nano Emulsions are consignment methods that improve the solubility and distribution of lipid medicines to the intended areas. SNEDDS of Itraconazole were developed using Castor oil, Tween 20 as surfactant and PEG 200 as co-surfactant. SNEDDS formulation can be obtained through phase diagram approach. Pseudo Ternary phase diagrams were constructed, using Chemix software, to optimize the concentrations of excipients. Thermodynamic stability studies were satisfactory. Robustness to dilution did not exhibit phase separation and drug precipitation. The Among 4 formulations, B1F3 formulation showed more than 95% of drug content and were considered superior and subjected to droplet size analysis and zeta potential measurement. Droplet size ranged from 120 nm to 505 nm. The Nano size was obtained for formulation. The zeta-potential results indicated the range -35 mV. Based on all evaluation tests, formulation B2F3 was chosen as the best. Thus, this self-Nano Emulsifying drug delivery system should be an effective oral dosage form for improving oral bioavailability of lipophilic drug Itraconazole.

Impact of carrier hydrophilicity on solid self nano-emulsifying drug delivery system and self nano-emulsifying granule system

The purpose of this study was to investigate the impact of carrier hydrophilicity on solid self nano-emulsifying drug delivery system (SNEDDS) and self nano-emulsifying granule system (SEGS). The mesoporous calcium silicate (Ca-silicate) and hydroxypropyl-β-cyclodextrin (HP-β-CD) were utilised as hydrophobic carrier and hydrophilic carrier, respectively. The liquid SNEDDS formulation, composed of Tween80/Kollipohr EL/corn oil (35/50/15%) with 31% (w/w) dexibuprofen, was spray-dried and fluid-bed granulated together with Avicel using Ca-silicate or HP- β-CD as a solid carrier, producing four different solid SNEDDS and SEGS formulations. Unlike the Ca-silicate-based systems, spherical shape and aggregated particles were shown in HP-β-CD-based solid SNEDDS and SEGS, respectively. Molecular interaction was detected between Ca-silicate and the drug; though, none was shown between HP-β-CD and the drug. Each system prepared with either carrier gave no significant differences in micromeritic properties, crystallinity, droplet morphology, size, dissolution and oral bioavailability in rats. However, the HP-β-CD-based system more significantly improved the drug solubility than did the Ca-silicate-based system. Therefore, both carriers hardly affected the properties of both solid SNEDDS and SEGS; though, there were differences in the aspect of appearance, molecular interaction and solubility.