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International Journal of Nanomedicine 2023The aim of this study was to develop a liposome gel containing -tetrahydropalmatine (-THP) and evaluate its transdermal properties.
PURPOSE
The aim of this study was to develop a liposome gel containing -tetrahydropalmatine (-THP) and evaluate its transdermal properties.
METHODS
A L (4) orthogonal experiment was conducted to optimize the preparation of -THP liposomes and assess their characterization and stability in a gel. The transdermal features were analyzed through in vivo and in vitro experiments on rats and Strat-M membrane, respectively. The metabolism of -THP in liver and skin S9 fractions was also studied.
RESULTS
The optimization of the orthogonal experiment revealed that the ideal mass ratio of phosphatidylcholine, cholesterol, and -THP during preparation was 10:1:3. The resulting liposome exhibited a particle size of 68 nm, a PDI of 0.27, a drug loading of 4.33%, an encapsulation of 18.79%, and a zeta potential of -41.27 mV. Both the -THP and its liposome-gel formulation were found to be stable for a duration of 45 days at 4 °C and 30 °C. During the in vivo transdermal study, the maximum concentration (C) of -THP from the liposome gel was 0.16 μg/mL, and the time to reach this maximum concentration (t) was 1.2 hours. The relative bioavailability of -THP in the liposome gel was 233.8% compared to the emulsion. The concentration of -THP (prepared in PBS) decreased at a rate of 0.0067 μg/mL/min in the liver S9 fraction and 0.0027 μg/mL/min in the skin S9 fraction, however, this difference was not observed when -THP was encapsulated in liposomes. -THP passed through the Strat-M membrane at a rate of 0.0032 mg/cm/h and 0.002 mg/cm/h for the emulsion and liposome gel, respectively.
CONCLUSION
The optimal process for the preparation of -THP liposomes was obtained. Compared to the emulsion, the liposomes provided greater bioavailability when used transdermally. The liposomes also provided greater stability for -THP during storage.
Topics: Animals; Rats; Liposomes; Emulsions; Skin; Lecithins
PubMed: 37600118
DOI: 10.2147/IJN.S422305 -
Medicine Sep 2022Localized senile pruritus is a continued health problem for the elderly. This study aimed to evaluate the efficacy and safety of artemether emulsion on localized senile... (Randomized Controlled Trial)
Randomized Controlled Trial
BACKGROUND
Localized senile pruritus is a continued health problem for the elderly. This study aimed to evaluate the efficacy and safety of artemether emulsion on localized senile pruritus.
METHODS
Sixty patients diagnosed with senile pruritus were randomized into the artemether emulsion (1%) group or emulsion base group in a 1:1 ratio (the artemether group vs the control group). The patients used artemether emulsion or emulsion base for pruritus twice daily for 2 weeks. The pruritus visual analog scale (VAS) and the rate of adverse events were evaluated in week 0 and week 2.
RESULTS
The VAS scores in week 2 after treatment decreased significantly compared with those before treatment in both groups (P < .05). After treatment, patients receiving the artemether emulsion had significantly lower mean VAS scores compared to those who received the emulsion base (1.21 ± 1.64 vs 3.67 ± 2.97, P < .05). When the VAS scores were compared between the 2 groups before treatment, the effective rate of the artemether group was significantly higher than that of the control group (χ2 = 55, P < .05) in week 2 after treatment. Besides, no adverse events occurred in both groups.
CONCLUSIONS
Both artemether emulsion and emulsion base were effective in treating localized senile pruritus, and artemether emulsion was superior to emulsion base.
Topics: Aged; Artemether; Emulsions; Humans; Pilot Projects; Pruritus; Visual Analog Scale
PubMed: 36107571
DOI: 10.1097/MD.0000000000030472 -
Critical Care (London, England) Jul 2014The use of intravenous lipid emulsions (ILEs) as antidote in local anaesthetic systemic toxicity has gained widespread support following convincing data from animal... (Review)
Review
The use of intravenous lipid emulsions (ILEs) as antidote in local anaesthetic systemic toxicity has gained widespread support following convincing data from animal models, and successful case reports in humans. Proposed beneficial mechanisms of action for ILEs include intravascular sequestration of intoxicant and subsequent enhanced redistribution to biologically inert tissues, augmentation of fatty acid utilisation for ATP synthesis in the context of metabolic poisoning, and direct cardiotonic and ion channel effects. The evidence base for use of ILEs in acute drug intoxication is evolving. The present evidence supports use of ILEs only in local anaesthetic systemic toxicity and in lipophilic cardiotoxin intoxication when there is an immediate threat to life, and other therapies have proven ineffective.
Topics: Animals; Fat Emulsions, Intravenous; Humans; Poisoning; Resuscitation
PubMed: 25673255
DOI: 10.1186/s13054-014-0457-5 -
Molecules (Basel, Switzerland) Oct 2023Cannabidiol (CBD) is a promising natural agent for treating psoriasis. CBD activity is attributed to inhibition of NF-kB, IL-1β, IL-6, and IL-17A. The present study...
Cannabidiol (CBD) is a promising natural agent for treating psoriasis. CBD activity is attributed to inhibition of NF-kB, IL-1β, IL-6, and IL-17A. The present study evaluated the anti-psoriatic effect of cannabidiol in lipid-stabilized nanoparticles (LSNs) using an imiquimod (IMQ)-induced psoriasis model in mice. CBD-loaded LSNs were stabilized with three types of lipids, Cetyl alcohol (CA), Lauric acid (LA), and stearic-lauric acids (SALA), and were examined in-vitro using rat skin and in-vivo using the IMQ-model. LSNs loaded with coumarin-6 showed a localized penetration depth of about 100 µm into rat skin. The LSNs were assessed by the IMQ model accompanied by visual (psoriasis area severity index; PASI), histological, and pro-psoriatic IL-17A evaluations. Groups treated with CBD-loaded LSNs were compared to groups treated with CBD-containing emulsion, unloaded LSNs, and clobetasol propionate, and to an untreated group. CBD-loaded LSNs significantly reduced PASI scoring compared to the CBD emulsion, the unloaded LSNs, and the untreated group (negative controls). In addition, SALA- and CA-containing nanoparticles significantly inhibited IL-17A release, showing a differential response: SALA > CA > LA. The data confirms the effectiveness of CBD in psoriasis therapy and underscores LSNs as a promising platform for delivering CBD to the skin.
Topics: Mice; Rats; Animals; Interleukin-17; Cannabidiol; Emulsions; Psoriasis; Skin; Imiquimod; Nanoparticles; Lipids; Disease Models, Animal; Mice, Inbred BALB C
PubMed: 37836750
DOI: 10.3390/molecules28196907 -
International Journal of Nanomedicine 2024Therapeutic proteins and peptides offer great advantages compared to traditional synthetic molecular drugs. However, stable protein loading and precise control of...
BACKGROUND
Therapeutic proteins and peptides offer great advantages compared to traditional synthetic molecular drugs. However, stable protein loading and precise control of protein release pose significant challenges due to the extensive range of physicochemical properties inherent to proteins. The development of a comprehensive protein delivery strategy becomes imperative accounting for the diverse nature of therapeutic proteins.
METHODS
Biodynamers are amphiphilic proteoid dynamic polymers consisting of amino acid derivatives connected through pH-responsive dynamic covalent chemistry. Taking advantage of the amphiphilic nature of the biodynamers, PNCs and DEs were possible to be prepared and investigated to compare the delivery efficiency in drug loading, stability, and cell uptake.
RESULTS
As a result, the optimized PNCs showed 3-fold encapsulation (<90%) and 5-fold loading capacity (30%) compared to DE-NPs. PNCs enhanced the delivery efficiency into the cells but aggregated easily on the cell membrane due to the limited stability. Although DE-NPs were limited in loading capacity compared to PNCs, they exhibit superior adaptability in stability and capacity for delivering a wider range of proteins compared to PNCs.
CONCLUSION
Our study highlights the potential of formulating both PNCs and DE-NPs using the same biodynamers, providing a comparative view on protein delivery efficacy using formulation methods.
Topics: Peptides; Emulsions; Humans; Proteins; Drug Delivery Systems; Polymers; Nanoparticles; Hydrogen-Ion Concentration; Amino Acids; Drug Carriers; Drug Liberation; Cell Survival
PubMed: 38784761
DOI: 10.2147/IJN.S448578 -
Journal of Colloid and Interface Science May 2020Cytotoxic drugs tend to have substantial side effects on healthy tissues leading to systemic toxicity, limited tolerated doses and reduced drug efficacy. A prominent...
Cytotoxic drugs tend to have substantial side effects on healthy tissues leading to systemic toxicity, limited tolerated doses and reduced drug efficacy. A prominent research area focuses on encapsulating cytotoxic drugs for targeted delivery to cancer tissues. However, existing carriers suffer from low drug loading levels and high drug leaching both when circulating systemically and when accumulating in non-target organs. These challenges mean that only few encapsulation technologies for delivery of cytotoxic drugs have been adopted for clinical use. Recently, we have demonstrated efficient manufacture of impermeable metal-shell/liquid core microcapsules that permit localised delivery by triggering release with ultrasound. This method has the potential to improve on existing methods for localised drug delivery because it:We demonstrate here the further miniaturization of both the emulsion droplet template and the thickness of the surrounding metal shell to the nanoscale in an attempt to take advantage of the EPR effect and the excretion of nanoparticles by the hepatobiliary system.
Topics: Antineoplastic Agents, Phytogenic; Drug Carriers; Drug Delivery Systems; Emulsions; Humans; Metal Nanoparticles; Paclitaxel; Particle Size; Platinum; Surface Properties
PubMed: 32045739
DOI: 10.1016/j.jcis.2019.12.018 -
Molecules (Basel, Switzerland) Aug 2021Ultrasonically synthesized core-shell microcapsules can be made of synthetic polymers or natural biopolymers, such as proteins and polysaccharides, and have found...
Ultrasonically synthesized core-shell microcapsules can be made of synthetic polymers or natural biopolymers, such as proteins and polysaccharides, and have found applications in food, drug delivery and cosmetics. This study reports on the ultrasonic synthesis of microcapsules using unmodified (natural) and biodegradable glycogen nanoparticles derived from various sources, such as rabbit and bovine liver, oyster and sweet corn, for the encapsulation of soybean oil and vitamin D. Depending on their source, glycogen nanoparticles exhibited differences in size and 'bound' proteins. We optimized various synthetic parameters, such as ultrasonic power, time and concentration of glycogens and the oil phase to obtain stable core-shell microcapsules. Particularly, under ultrasound-induced emulsification conditions (sonication time 45 s and sonication power 160 W), native glycogens formed microcapsules with diameter between 0.3 μm and 8 μm. It was found that the size of glycogen as well as the protein component play an important role in stabilizing the Pickering emulsion and the microcapsules shell. This study highlights that native glycogen nanoparticles without any further tedious chemical modification steps can be successfully used for the encapsulation of nutrients.
Topics: Animals; Biopolymers; Capsules; Cattle; Drug Delivery Systems; Emulsions; Glycogen; Nanoparticles; Polymers; Polysaccharides; Rabbits; Sonication; Soybean Oil; Ultrasonics; Vitamin D
PubMed: 34500590
DOI: 10.3390/molecules26175157 -
Biomaterials Jun 2019Catheter-based intra-arterial drug therapies have proven effective for a range of oncologic, neurologic, and cardiovascular applications. However, these procedures are...
Catheter-based intra-arterial drug therapies have proven effective for a range of oncologic, neurologic, and cardiovascular applications. However, these procedures are limited by their invasiveness and relatively broad drug spatial distribution. The ideal technique for local pharmacotherapy would be noninvasive and would flexibly deliver a given drug to any region of the body with high spatial and temporal precision. Combining polymeric perfluorocarbon nanoemulsions with existent clinical focused ultrasound systems could in principle meet these needs, but it has not been clear whether these nanoparticles could provide the necessary drug loading, stability, and generalizability across a range of drugs, beyond a few niche applications. Here, we develop polymeric perfluorocarbon nanoemulsions into a generalized platform for ultrasound-targeted delivery of hydrophobic drugs with high potential for clinical translation. We demonstrate that a wide variety of drugs may be effectively uncaged with ultrasound using these nanoparticles, with drug loading increasing with hydrophobicity. We also set the stage for clinical translation by delineating production protocols that are scalable and yield sterile, stable, and optimized ultrasound-activated drug-loaded nanoemulsions. Finally, we exhibit a new potential application of these nanoemulsions for local control of vascular tone. This work establishes the power of polymeric perfluorocarbon nanoemulsions as a clinically-translatable platform for efficacious, noninvasive, and localized ultrasonic drug uncaging for myriad targets in the brain and body.
Topics: Drug Delivery Systems; Emulsions; Fluorocarbons; Nanoparticles; Polymers
PubMed: 30953907
DOI: 10.1016/j.biomaterials.2019.03.021 -
International Journal of Pharmaceutics Jan 2023Drug-loaded emulsions for spray drying should be optimised for their rheological behaviour and stability under operating conditions, as this is essential for achieving...
Drug-loaded emulsions for spray drying should be optimised for their rheological behaviour and stability under operating conditions, as this is essential for achieving the desired physicochemical properties of the final dry product. Our aim was therefore to investigate the structure and stability of a water-in-oil (W/O) emulsion containing vancomycin hydrochloride as the active ingredient in the aqueous phase, poly(d,l-lactide-co-glycolide) as the structural polymer in the dichloromethane-based organic phase, and various stabilisers using low-field nuclear magnetic resonance (LF NMR) and rheological characterisation. Four emulsions were tested, namely-one without stabiliser, one with Poloxamer® 407, one with chitosan and Span™ 80 and one with chitosan only. The theoretical interpretation of the rheological data allowed the determination of the velocity and the shear rate/stress profiles inside the feed path of the W/O emulsion, aspects that are critical for the industrial scale-up of the emulsion drying process. In addition, LF NMR demonstrated that shaking was sufficient to restore the original emulsion structure and that the droplet size of all emulsions was in the range of 1-10 μm, although the emulsion with chitosan had the narrowest droplet size distribution and the higher zero shear viscosity, which accounts for the increased long-term stability due to impeded droplets movement.
Topics: Water; Polylactic Acid-Polyglycolic Acid Copolymer; Emulsions; Spray Drying; Chitosan; Magnetic Resonance Spectroscopy; Rheology; Particle Size
PubMed: 36509222
DOI: 10.1016/j.ijpharm.2022.122471 -
International Journal of Molecular... Jan 2021(1) Background: Chiral nanoparticular systems have recently emerged as a compelling platform for investigating stereospecific behavior at the nanoscopic level. We...
(1) Background: Chiral nanoparticular systems have recently emerged as a compelling platform for investigating stereospecific behavior at the nanoscopic level. We describe chiroselective supramolecular interactions that occur between DNA oligonucleotides and chiral polyurea nanocapsules. (2) Methods: We employ interfacial polyaddition reactions between toluene 2,4-diisocyanate and lysine enantiomers that occur in volatile oil-in-water nanoemulsions to synthesize hollow, solvent-free capsules with average sizes of approximately 300 nm and neutral surface potential. (3) Results: The resultant nanocapsules exhibit chiroptical activity and interact differentially with single stranded DNA oligonucleotides despite the lack of surface charge and, thus, the absence of significant electrostatic interactions. Preferential binding of DNA on D-polyurea nanocapsules compared to their L-counterparts is demonstrated by a fourfold increase in capsule size, a 50% higher rise in the absolute value of negative zeta potential (ζ-potential), and a three times lower free DNA concentration after equilibration with the excess of DNA. (4) Conclusions: We infer that the chirality of the novel polymeric nanocapsules affects their supramolecular interactions with DNA, possibly through modification of the surface morphology. These interactions can be exploited when developing carriers for gene therapy and theranostics. The resultant constructs are expected to be highly biocompatible due to their neutral potential and biodegradability of polyurea shells.
Topics: Aptamers, Nucleotide; DNA; Drug Carriers; Emulsions; Humans; Nanocapsules; Oligonucleotides; Particle Size; Polymers
PubMed: 33430158
DOI: 10.3390/ijms22020584