Chitosan nanoparticles loading oxaliplatin as a mucoadhesive topical treatment of oral tumors: Iontophoresis further enhances drug delivery ex vivo

Topical ophthalmic antibiotics show low efficacy due to the well-known physiological defense mechanisms of the eye, which prevents the penetration of exogenous substances. Here, we aimed to incorporate besifloxacin into liposomes containing amines as positively charged additives and to evaluate the influence of this charge on drug delivery in two situations: (i) iontophoretic and (ii) passive treatments. Hypothesis are (i) charge might enhance the electromigration component upon current application improving penetration efficiency for a burst drug delivery, and (ii) positive charge might prolong formulation residence time, hence drug penetration. Liposomes elaborated with phosphatidylcholine (LP PC) or phosphatidylcholine and spermine (LP PC: SPM) were stable under storage at 6 ºC for 30 days, showed mucoadhesive characteristics, and were non-irritant, according to HET-CAM tests. Electron paramagnetic resonance spectroscopy measurements showed that neither the drug nor spermine incorporations produced evident alterations in the fluidity of the liposome's membranes, which retained their structural stability even under iontophoretic conditions. Mean diameter and zeta potential were 177.2 ± 2.7 nm and − 5.7 ± 0.3 mV, respectively, for LP PC; and 175.4 ± 1.9 nm and + 19.5 ± 1.0 mV, respectively, for LP PC:SPM. The minimal inhibitory concentration (MIC) and the minimal bactericide concentration (MBC) of the liposomes for P. aeruginosa showed values lower than the commercial formulation (Besivance). Nevertheless, both formulations presented a similar increase in permeability upon the electric current application. Hence, liposome charge incorporation did not prove to be additionally advantageous for iontophoretic therapy. Passive drug penetration was evaluated through a novel in vitro ocular model that simulates the lacrimal flow and challenges the formulation resistance in the passive delivery situation. As expected, LP PC: SPM showed higher permeation than the control (Besivance). In conclusion, besifloxacin incorporation into positively charged liposomes improved passive topical delivery and can be a good strategy to improve topical ophthalmic treatments.

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“…Mucoadhesiveness was evaluated in vitro 31 . Briefly, mucin type III was hydrated with ultrapure water (1:10 w/v) overnight.…”

Section: Preparation Of Liposomal Formulationsmentioning

confidence: 99%

Besifloxacin liposomes with positively charged additives for an improved topical ocular delivery

Santos

Ferreira‐Nunes

Dalmolin

et al. 2020

Sci Rep

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“…Ex‐vivo studies showed that the use of chitosan increases 3‐fold the drug penetration through oral mucosa. In addition, the number of apoptotic cells increased in the presence of chitosan nanoparticles [62] . Another study shows the development of chitosan nanoparticles through ionic gelation by electrostatic interaction between chitosan and carboxymethyl‐chitosan.…”

Section: Polysaccharides In Drug Deliverymentioning

confidence: 96%

Polysaccharide Chemistry in Drug Delivery, Endocrinology, and Vaccines

Khalid

Asim-ur-Rehman

Ahmed

et al. 2021

Chemistry A European J

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Polysaccharides, due to their outstanding properties, have attracted the attention of researchers, working in the biomedical field and especially of those working in drug delivery. Modified/functionalized polysaccharides further increase the importance for various applications. Delivery of therapeutics for diverse ailments in different endocrine glands and hormones safely, is a focal point of researchers working in the field. Among the routes followed, the transdermal route is preferred due to non‐exposure of active moieties to the harsh gastric environment and first‐pass metabolism. This review starts with the overview of polysaccharides used for the delivery of various therapeutic agents. Advantages of polysaccharides used in the transdermal route are addressed in detail. Types of polysaccharides will be elaborated through examples, and in this context, special emphasis will be on the polysaccharides being used for synthesis of the membranes/films. Techniques employed for their modification to design novel carriers for therapeutics delivery will also be discussed. The review will end with a brief discussion on recent developments and future perspectives for delivery of therapeutic agents, and vaccine development.

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“…Like skin, the buccal mucosa is an attractive site for immunization. One study tested the effectiveness of a microneedle array for immunization via murine buccal mucosa [ 131 ]. Solid microneedles in an array were coated with ovalbumin, and the microneedle array was applied to murine buccal mucosa twice two weeks apart.…”

Section: Buccal Absorptionmentioning

confidence: 99%

Roles of Lipids in the Permeability Barriers of Skin and Oral Mucosa

Wertz

2021

IJMS

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PubMed searches reveal much literature regarding lipids in barrier function of skin and less literature on lipids in barrier function of the oral mucosa. In terrestrial mammals, birds, and reptiles, the skin’s permeability barrier is provided by ceramides, fatty acids, and cholesterol in the outermost layers of the epidermis, the stratum corneum. This layer consists of about 10–20 layers of cornified cells embedded in a lipid matrix. It effectively prevents loss of water and electrolytes from the underlying tissue, and it limits the penetration of potentially harmful substances from the environment. In the oral cavity, the regions of the gingiva and hard palate are covered by keratinized epithelia that much resemble the epidermis. The oral stratum corneum contains a lipid mixture similar to that in the epidermal stratum corneum but in lower amounts and is accordingly more permeable. The superficial regions of the nonkeratinized oral epithelia also provide a permeability barrier. These epithelial regions do contain ceramides, cholesterol, and free fatty acids, which may underlie barrier function. The oral epithelial permeability barriers primarily protect the underlying tissue by preventing the penetration of potentially toxic substances, including microbial products. Transdermal drug delivery, buccal absorption, and lipid-related disease are discussed.

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Chitosan nanoparticles loading oxaliplatin as a mucoadhesive topical treatment of oral tumors: Iontophoresis further enhances drug delivery ex vivo

Cited by 78 publications

References 40 publications

Besifloxacin liposomes with positively charged additives for an improved topical ocular delivery

Besifloxacin liposomes with positively charged additives for an improved topical ocular delivery

Polysaccharide Chemistry in Drug Delivery, Endocrinology, and Vaccines

Roles of Lipids in the Permeability Barriers of Skin and Oral Mucosa

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