Therapeutic Delivery

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Aim: This investigation aimed to develop a voriconazole-loaded chitosan-coated cationic microemulsion (CVME) to treat fungal keratitis. Methods: Microemulsions were prepared using water titration, and the optimized microemulsion was coated with chitosan to prepare CVME. The physicochemical parameters, ocular irritation potential, in vitro antifungal efficacy and in vitro release studies were performed. The in vivo antifungal efficacy study was conducted in a fungal infection-induced rabbit eye model. Results: The developed CVME displayed acceptable physicochemical properties and excellent mucoadhesive behavior and showed a sustained release profile...

Aim: The novel hydrogel systems made from sodium alginate, pectin, beta-cyclodextrin and deoxycholic acid (DCA) were proposed as potential drug-delivery matrices. Materials & methods: To ensure biocompatibility, rheological parameters were examined and hydrogels' effects on bioenergetic parameters and cellular viability on murine hepatic, and muscle and pancreatic beta cells. Results & conclusion: All hydrogels show non-Newtonian, shear thinning behavior. Cells displayed various oxygen-dependent viability patterns, with the bile acid overall adversely affecting their biological activities...

Aim: The aim of this study is to test the biocompatibility of hydrogels with polysaccharides and bile acids on three murine cell lines. Materials & methods: Novel hydrogels containing poloxamer 407, polysaccharides (starch, pectin, acacia, carboxymethyl and methyl 2-hydroxyethyl cellulose) and deoxycholic acid were prepared using cold method, sterilized and used in biological assays to determine effects on hepatic, muscle, and pancreatic beta cells. Results and conclusion: Hydrogels with deoxycholic acid had tissue-depending effects on cellular survival and bioenergetics, resulting in the best cellular viability and bioenergetics within pancreatic beta cells...

Aim: The study aimed to develop and evaluate an aquasome drug-delivery system for controlled drug delivery of cefprozil monohydrate. Materials & methods: Aquasomes were prepared by the spinal method with a calcium phosphate core, sugar-coated using cellobiose and drug-loaded by adsorption. The formulations were characterized for size, morphology and drug release. An antibacterial study was conducted for Gram-positive and -negative bacteria. Results: It showed particle size of 2791.9 nm, zeta potential of -0...

The treatment of fungal infections is challenging with high death rates reported among immunocompromised patients. The currently available antifungals suffer from poor bioavailability and solubility, pharmacokinetics, and drug resistance, with limited cellular uptake. The clinical pipeline of new antifungals is dry. The incorporation of antifungal drugs into polymer-based nanocarriers to form nanotherapeutics is a promising approach to enhance the therapeutic outcomes of the available antifungal drugs. This review summarizes different polymer-based nanotherapeutics strategies that have been explored for the delivery of antifungals, resulting in enhanced therapeutic outcomes, such as improved pharmacokinetics, targeted/sustained delivery, prolonged drug circulation, retention of the drugs at the localized site of action, and overcoming drug resistance when compared with the free antifungal drugs...

Aim: Design of moxifloxacin and ornidazole co-loaded polycaprolactone and gelatin nanofiber dressing for diabetic wounds. Materials & methods: The composite nanofibers were prepared using electrospinning technique and characterized for in vitro drug release, antibacterial activity, laser doppler and in vivo wound healing. Results: The optimized nanofiber demonstrated an interconnected bead free nanofiber with average diameter <200 nm. The in vitro drug release & antimicrobial studies revealed that optimized nanofiber provided drug release for >120 h, thereby inhibiting growth of Escherichia coli and Stapyhlococcus aureus ...

During the past few decades, researchers have attempted to discover an effective treatment for cancer. Exosomes are natural nanovesicles released by various cells and play a role in communication between cells. While natural exosomes have high clinical potential, their inherent limitations have prompted researchers to design exosomes with improved therapeutic properties. To achieve this purpose, researchers have undertaken exosome engineering to modify the surface properties or internal composition of exosomes...

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Biopharmaceutical products are currently well-established in nearly all branches of medicine and are believed to have great potential for the treatment of a broad spectrum of diseases. Peptide/protein drugs exhibit a predominant class of new biopharmaceuticals coming on the market in recent years. Oral delivery of peptides/proteins as a non-invasive therapeutic technique has become an appealing alternative to the parenteral route. However, the efficient oral delivery of peptides/proteins is limited because of their high molecular weight, poor stability and low biodistribution...

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Naringenin belongs to the flavanones and is mainly found in fruits (grapefruit and oranges) and vegetables. Naringenin exhibits lipid-lowering and insulin-like characteristics and is used to treat osteoporosis, cancer and cardiovascular disorders. Their incorporation into drug formulations offers several advantages, including enhanced solubility, improved bioavailability and targeted delivery. Naringin-based formulations are beneficial in cancer, for example controlling breast and prostate cancer by inhibition of CYP19...

Aim: Inhalable microspheres made of polymers as a targeted drug delivery system have been developed to overcome the limitation of current treatments in Tuberculosis. Materials & methods: Isoniazid inhalable microspheres were created using a gelation ionotropic method with sodium alginate, carrageenan and calcium chloride in four different formulations. Result: The particle morphology has smooth surfaces and round spherical shapes with sizes below 5 μm; good flowability. The drug loading and entrapment efficiency values ranged from 1...

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Aim: Atazanavir sulphate belongs to BCS class II drug, its oral bioavailability is limited due to its rapid first-pass metabolism and P-gp efflux. Materials & methods: The in situ floating gel using the complexed drug was prepared by ion gelation method and optimized the formulation as per 32 full factorial design. Results: Floating lag time of optimized formulation was found to be 18 s and percentage drug release of 94.18 ± 0.18 % at the end of 16 h. The concentration of gelling polymer affects drug release and a floating lag time and vice versa ...

Aim: Obesity is a chronic pathology of epidemic proportions. Mature adipocytes from a 3T3-L1 cell line were used as in vitro obesity model to test different bioactive compounds. We aim to evaluate cassis ( Ribes nigrum ) extract antioxidant activity and its antiadipogenic effect on mature adipocytes. Results: We produced an extract by using enzyme that combines cellulase and pectinase; we obtained high yield of the bioactive compound anthocyanin. Extract showed high antioxidant capacity. We conducted in vitro assays by adding the extract to adipocytes culture medium...

Aim: Gefitinib-loaded D-α-tocopherol polyethylene glycol 1000 succinate (TPGS)-coated cationic liposomes (GEF-TPGS-LIPO+ ) were developed and optimized by the quality by design (QbD) approach for its potential anticancer effect. Methods/materials: Box-Behnken design (BBD) a systematic design of experiments was added to screen and optimize the formulation variables. Results: GEF-TPGS-LIPO+ shows vesicle size (210 ± 4.82 nm), polydispersity index (0.271 ± 0.002), zeta potential (22...

Aim: To develop a propranolol HCL-loaded liposomal nasal formulation for migraine prophylaxis. Materials & methods: Formulated the liposomes through thin layer hydration method and optimized via design of experiments (DOE). The prepared liposomes were characterized for particle size, zeta potential, PDI, drug entrapment and drug loading. Assessed for in vitro release kinetics, ex vivo permeability, histopathology and stability. Results: Optimized liposomes: 135.52 ± 5...

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Recently, the role of inorganic ions has been explored for its wound-healing applications. Ions do play key role in the normal functioning of the skin, including the epidermal barrier property, maintaining redox balance, enzymatic activities, tissue remodeling, etc. The care of chronic wounds is a concern and new cost-effective therapeutic strategies that modulate the wound microenvironment and cell behaviour are needed. First, this review illustrates the ions that play a role in wound healing and their molecular mechanisms that are accountable for modifying the wound...