Topical Delivery of Meloxicam using Liposome and Microemulsion Formulation Approaches

Zhang, Julia; Froelich, Anna; Michniak‐Kohn, Bozena

doi:10.3390/pharmaceutics12030282

Cited by 41 publications

(35 citation statements)

References 66 publications

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“…Particle diameters of 10−200 nm are most relevant for exerting biological effects [ 33 ]. For lipid-based nanoparticles, a PDI of ≤ 0.3 is considered to be acceptable [ 34 ]. Our nanosystems showed a PDI of 0.42, and they can be considered highly polydisperse [ 35 ].…”

Section: Discussionmentioning

confidence: 99%

Multifunctional lipid-based nanocarriers with antibacterial and anti‐inflammatory activities for treating MRSA bacteremia in mice

Liao

Yang

et al. 2021

J Nanobiotechnol

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Background Bacteremia-induced sepsis is a leading cause of mortality in intensive care units. To control a bacterial infection, an immune response is required, but this response might contribute to organ failure. Kidneys are one of the main organs affected by bacteremia. Combination therapies with antibacterial and anti-inflammatory effects may be beneficial in treating bacteremia. This study aimed to develop nanostructured lipid carriers (NLCs) loaded with ciprofloxacin and rolipram that exert a combination of anti-methicillin-resistant Staphylococcus aureus (MRSA) and anti-inflammatory effects. Retinol was incorporated into the nanoparticles to transport retinol-binding protein 4 (RBP4) to the kidneys, which abundantly express RBP receptors. The NLCs were fabricated by high-shear homogenization and sonication, and neutrophils were used as a model to assess their anti-inflammatory effects. Mice were injected with MRSA to establish a model of bacteremia with organ injury. Results The mean nanoparticle size and zeta potential of the NLCs were 171 nm and − 39 mV, respectively. Ciprofloxacin (0.05%, w/v) and rolipram (0.02%) achieved encapsulation percentages of 88% and 96%, respectively, in the nanosystems. The minimum bactericidal concentration of free ciprofloxacin against MRSA increased from 1.95 to 15.63 µg/ml when combined with rolipram, indicating a possible drug-drug interaction that reduced the antibacterial effect. Nanoparticle inclusion promoted the anti-MRSA activity of ciprofloxacin according to time-kill curves. The NLCs were found to be largely internalized into neutrophils and exhibited superior superoxide anion inhibition than free drugs. Retinol incorporation into the nanocarriers facilitated their efficient targeting to the kidneys. The NLCs significantly mitigated MRSA burden and elastase distribution in the organs of MRSA-infected animals, and the greatest inhibition was observed in the kidneys. Bacterial clearance and neutrophil infiltration suppression attenuated the bacteremia-induced cytokine overexpression, leading to an improvement in the survival rate from 22% to 67%. Conclusions The dual role of our NLCs endowed them with greater efficacy in treating MRSA bacteremia than that of free drugs.

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Section: Discussionmentioning

confidence: 99%

Multifunctional lipid-based nanocarriers with antibacterial and anti‐inflammatory activities for treating MRSA bacteremia in mice

Liao

Yang

et al. 2021

J Nanobiotechnol

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“…The formulations developed in the previous studies 14,15 had low MX content, so the resulting gel formulations did not yield any meaningful permeation results. Therefore, we modified the liposomal formulations as summarized in Table 1 in the present study to increase the content of MX.…”

Section: Characterization Of Mx-loaded Liposomesmentioning

confidence: 92%

“…In order to improve its solubility and lipophilicity, one of the available options is to encapsulate the MX in a liposomal formulation that will improve the solubility and permeability through Stratum corneum . In our previous studies, we have used both transfersomes 14 and flavosomes 15 to encapsulate MX and observed improved solubility and skin permeability of MX into the deeper layers of human skin. Transfersomes are considered the first generation of deformable vesicles developed by Cevc and Blume 16 and Cevc et al, 17 They are generally prepared by addition of a surfactant (edge activator) into the conventional liposomes.…”

Section: Introductionmentioning

confidence: 99%

<p>Deformable Liposomal Hydrogel for Dermal and Transdermal Delivery of Meloxicam</p>

Zhang¹,

Osmałek²,

Michniak‐Kohn³

2020

IJN

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Background and Aim: Meloxicam (MX) is a potent hydrophobic non-steroidal antiinflammatory drug used to reduce inflammation and pain. However, its oral dosage form can cause many adverse gastrointestinal effects. In the present study, a poloxamer P407 based hydrogel system containing transfersomes or flavosomes has been prepared as a potential therapeutic vehicle for the topical delivery of MX. Methods: In this study, MX was encapsulated in conventional liposomes, transfersomes, and flavosomes. The obtained liposomal vesicles were characterized in terms of size, drug entrapment efficiency, zeta potential, and stability. These MX-loaded liposomal formulations were further incorporated into a poloxamer P407 gel and evaluated using rheological properties, a stability study and an ex vivo permeation study through human cadaver skin by both HPLC analysis and confocal laser scanning microscopy (CLSM). Results: The developed deformable liposomes exhibited homogeneous vesicle sizes less than 120 nm with a higher entrapment efficiency as compared to conventional liposomes. The deformable liposomal gel formulations showed improved permeability compared to a conventional liposomal gel and a liposome-free gel. The enhancement effect was also clearly visible by CLSM. Conclusion: These deformable liposomal hydrogel formulations can be a promising alternative to conventional oral delivery of MX by topical administration. Notably, flavosomeloaded gel formulations displayed the highest permeability through the deeper layers of the skin and shortened lag time, indicating a potential faster on-site pain relief and antiinflammatory effect.

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“…Under stress conditions, EA relocates in the areas with higher curvature. 25,26 Other types of liposomes can be prepared and characterized following the same methodology as for conventional liposomes, as will be discussed later.…”

Section: Ultradeformable Liposomesmentioning

confidence: 99%

“…The particle size is going to play an important role in terms of skin delivery because it affects the penetration of encapsulated compounds through the skin to the deeper layers. 26,40 MPPC, monopalmitoyl-2-hydroxy-sn-glycero-3-phosphocholine; P80, Polysorbate 80; PDI, Polydispersity Index; PC, phosphatidylcholine; SL, soybean lecithin; SPC, soy phosphatidylcholine; S80, Span 80; SC, sodium cholate; SM, sorbitan monooleate; T80, Tween 80; TEM, transmission electron microscopy; YL, yolk lecithin; w/w, weight/weight.…”

Section: Particle Size Reductionmentioning

confidence: 99%

<p>Development, Characterization and Use of Liposomes as Amphipathic Transporters of Bioactive Compounds for Melanoma Treatment and Reduction of Skin Inflammation: A Review</p>

Castañeda-Reyes

Perea-Flores

Dávila-Ortíz

et al. 2020

IJN

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The skin is the largest organ in the human body, providing a barrier to the external environment. It is composed of three layers: epidermis, dermis and hypodermis. The most external epidermis is exposed to stress factors that may lead to skin conditions such as photo-aging and skin cancer. Some treatments for skin disease utilize the incorporation of drugs or bioactive compounds into nanocarriers known as liposomes. Liposomes are membranes whose sizes range from nano to micrometers and are composed mostly of phospholipids and cholesterol, forming similar structures to cell membranes. Thus, skin treatments with liposomes have lower toxicity in comparison to traditional treatment routes such as parenteral and oral. Furthermore, addition of edge activators to the liposomes decreases the rigidity of the bilayer structure making it deformable, thereby improving skin permeability. Liposomes are composed of an aqueous core and a lipidic bilayer, which confers their amphiphilic property. Thus, they can carry hydrophobic and hydrophilic compounds, even simultaneously. Current applications of these nanocarriers are mainly in the cosmetic and pharmaceutic industries. Nevertheless, new research has revealed promising results regarding the effectiveness of liposomes for transporting bioactive compounds through the skin. Liposomes have been well studied; however, additional research is needed on the efficacy of liposomes loaded with bioactive peptides for skin delivery. The objective of this review is to provide an up-to-date description of existing techniques for the development of liposomes and their use as transporters of bioactive compounds in skin conditions such as melanoma and skin inflammation. Furthermore, to gain an understanding of the behavior of liposomes during the process of skin delivery of bioactive compounds into skin cells.

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Topical Delivery of Meloxicam using Liposome and Microemulsion Formulation Approaches

Cited by 41 publications

References 66 publications

Multifunctional lipid-based nanocarriers with antibacterial and anti‐inflammatory activities for treating MRSA bacteremia in mice

Multifunctional lipid-based nanocarriers with antibacterial and anti‐inflammatory activities for treating MRSA bacteremia in mice

<p>Deformable Liposomal Hydrogel for Dermal and Transdermal Delivery of Meloxicam</p>

<p>Development, Characterization and Use of Liposomes as Amphipathic Transporters of Bioactive Compounds for Melanoma Treatment and Reduction of Skin Inflammation: A Review</p>

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