Pharmaceutical Nanotechnology - Volume 10, Issue 5, 2022

Nanomaterials (NMs) have favorable application in the medicine area, specifically in regard to the carrying of pharmaceutical ingredients to provide targeted drug delivery systems. The skin is an excellent route for the delivery of pharmaceutical nano-transporters for skin-related applications. The physicochemical properties of nanomaterials such as size, hydrophobicity, loading capacity, charge and weight are vital for a skin penetrating system. Many nanocarriers such as polymeric nanoparticles, inorganic nanomaterials and, lipid nanostructures have been utilized for dermal delivery of active ingredients and others such as carbon nanotubes and fullerenes require more examination for future application in the skin-related area. Some negative side effects and nano-cytotoxicity of nanomaterials require special attention while investigating different nanomaterials for medicinal applications. Then, in the current review, we had a view on the safety issues of nanomaterials for dermal pharmaceutical products.

Pulmonary arterial hypertension (PAH) is an uncommon condition marked by elevated pulmonary artery pressure that leads to right ventricular failure. The majority of drugs are now being approved by FDA for PAH, however, several biopharmaceutical hindrances lead to failure of the therapy. Various novel drug delivery systems are available in the literature from which lipid-based nanoparticles i.e. solid lipid nanoparticle is widely investigated for improving the solubility and bioavailability of drugs. In this paper, the prototype phytoconstituents used in pulmonary arterial hypertension have limited solubility and bioavailability. We highlighted the novel concepts of SLN for lipophilic phytoconstituents with their potential applications. This paper also reviews the present state of the art regarding production techniques for SLN like High-Pressure Homogenization, Microemulsion Technique, and Phase Inversion Temperature Method, etc. Furthermore, toxicity aspects and in vivo fate of SLN are also highlighted in this review. In a nutshell, safer delivery of phytoconstituents by SLN added a novel feather to the cap of successful drug delivery technologies.

In recent years, nanotechnology has gained much attention from scientists for the obtainment of significant advances in therapeutic potential. Nano-delivery systems have emerged as an effective way to improve the therapeutic properties of drugs, including solubility, stability, prolongation of half-life, as well as promoting the accumulation of drug at the target site. The nanoparticles have also been incorporated into various conventional drug delivery systems. This review study aims to introduce the amalgamation of nanoparticles into drug carriers. To overcome the limitations of single nanoparticles, such as toxicity, high instability, rapid drug release as well as limited drug loading capacity, a multi-component system is developed. Liposomes, microparticles, nanofibers, dendrimers, etc., are promising drug carriers, having some limitations that can be minimized, and the compilation of nanoparticles synergizes the properties. The amalgamated nanocarriers are used for the diagnostic purpose as well as treatment of various chronic diseases. It also increases the solubility of hydrophobic drugs. However, each system has its advantages and disadvantages based on its physicochemical properties, efficacy, and other parameters. This review details the past and present state of development for the fusion of nanoparticles within drug carriers and future research works are needed for the same.

Lipid-based formulations have emerged as prospective dosage forms for extracting the therapeutic effects of existing lipophilic compounds and novel chemical entities more efficiently. Compared to other excipients, lipids have the added benefit of enhancing the bioavailability of lipophilic and highly metabolizable drugs due to their unique physicochemical features and similarities to in vivo components. Furthermore, lipids can minimize the needed dose and even the toxicity of drugs with poor aqueous solubility when employed as the primary excipient. Hence, the aim of the present review is to highlight the functional behavior of lipid excipients used in SNEDD formulation along with the stability aspects of the formulation in vivo. Moreover, this review also covered the importance of SNEDDS in drug delivery, the therapeutic and manufacturing benefits of lipids as excipients, and the technological advances made so far to convert liquid to solid SNEDDS like melt granulation, adsorption on a solid support, spray cooling, melt extrusion/ spheronization has also highlighted. The mechanistic understanding of SNEDD absorption in vivo is highly complex, which was discussed very critically in this review. An emphasis on their application and success on an industrial scale was presented, as supported by case studies and patent surveys.

Osteoporosis is characterised by a major public health burden, particularly taking into account the ageing global population. Therapeutic modalities for osteoporosis are categorised on the basis of their effect on bone remodeling: antiresorptive and anabolic agents. Anabolic drugs are favoured as they promote the formation of new bone, whereas antiresorptive drugs terminate the further deterioration of bone. Non-specific delivery of anabolic agents results in prolonged kidney exposure causing malignant hypercalcemia, whereas antiresorptive agents and bisphosphonates may produce osteonecrosis of the jaw. Several clinical trials have been reported for combinational therapy of anabolic agents and antiresorptive agents for osteoporosis. However, none of them have proven their cumulative effects in the treatment of disease. The present work emphasizes a dualtargeting drug delivery approach comprising of bone anabolic and antiresorptive agents that would simultaneously deliver the therapeutic agents to both the zones of bone. The anticipated pioneering delivery approach will intensify the explicit interaction between the therapeutic agent and bone surfaces separately without developing severe adverse effects and improve osteoporotic therapy effectively compared to non-targeted drug delivery.

Background: Levofloxacin is available in the form of an eye drop solution for the treatment of ocular bacterial infection and inflammatory diseases. Below 5% of the drug gets absorbed after topical application of eye drop. The major portion of administered drug either comes out from the eye or drains out by the nasolacrimal duct, which results in poor bioavailability. Objective: We aim to prepare a polymeric ocular insert containing levofloxacin as a drug prepared by the electrospinning technique that can release the drug for an extended duration. Methods: Electrospun nanofiber sheets were prepared using hydroxypropyl cellulose and polycaprolactone polymer. Drug content was analysed by HPLC. Nanosheet was examined by DSC and FTIR for compatibility study. Optimized nanosheet was further studied for weight uniformity, swellability index, surface pH, and in-vitro drug release. The morphology of the prepared sheets was examined using optical microscopy and SEM analysis. Results: The uniform, beadles, and continuous nanofibers were obtained by electrospinning. From the DSC and FTIR data, it was proved that drugs and polymers were compatible in nanosheets. Drug content and % drug loading in the electrospun sheets were found to be 101.70% and 4.33%, respectively. The thickness of the sheets was around 0.31± 0.04 mm and the swelling index was observed at 566.66% after 30 min. The surface pH of the ocular insert was found to be 6.81 and 6.83 after 30 min and 24 h., respectively. In-vitro drug release showed that 99% of the drug was released in 8 h. Conclusion: A prepared nanocomposite sheet can be used for the sustained drug delivery of levofloxacin in ocular eye disease, reducing the dosing frequency and improving patient compliance.

Introduction: Molybdenum (VI) oxide nanoparticles (MoO3 NPs) are widely used in various economic activities. This creates elevated risks of exposure to this nanomaterial for workers and the population in general, and consequently, there can be an increased number of developing pathological changes caused by exposure to MoO3 NPs. Objective: The study aims to examine and comparatively assess peculiarities of bioaccumulation and toxic effects produced by MoO NPs under multiple oral introductions. Methods: We evaluated the sizes of analyzed particles by scanning electronic microscopy; the specific surface area was calculated by the method of Brunauer, Emmett and Taylor; the total pore volume by Barrett, Joyner and Halenda. Rats were exposed as per the scheme introduced by Lim with colleagues. We examined biochemical and hematological blood indicators, molybdenum concentrations, and pathomorphological changes in tissues of various organs 24 hours after the last exposure. The study involved a comparison with effects produced by MoO3 microparticles. Results: The tested MoO3 sample was established to be a nanomaterial as per the whole set of its physical properties. 50% of animals in the exposed group died on the 16th day of the experiment after the total exposure dose of MoO3 NPs reached 6500 mg/kg of body weight. Having analyzed blood plasma, we determined the following. There was a growth in the quantity of leukocytes and a share of segmented neutrophils and monocytes, which were 1.76-3.50 times higher than in the control group. Activity of alanine aminotransferase, aspartate aminotransferase, alkaline phosphatase, gammaglutamyl transpeptidase, alpha-amylase, and lactate dehydrogenase, and concentrations of urea, crude and direct bilirubin was higher by 1.61-22.86 times. Decrease in the number of platelets, plateletcrit, the relative number of lymphocytes, and the number and proportion of large platelets by 1.31-2.71 times. We detected elevated molybdenum concentrations in the lungs, heart, liver, kidneys, brain, and blood under exposure to MoO3 NPs, exceeding the control values by 12.10-361.75 times. Rats exposed to MoO3 NPs had liver parenchymal steatosis, inflammatory changes, hemorrhagic infarctions, and hyperplasia in the lungs. Conclusion: MoO3 NPs are more able to bioaccumulate and produce toxic effects compared with their microdispersed analogue under multiple oral introductions into the body.