Pharmaceutical Nanotechnology - Volume 11, Issue 4, 2023

Nanomaterials are emerging as an innovative and efficient instrument for the transport and cellular translocation of therapeutic compounds, namely, biopharmaceuticals. The use of nanoparticles as drug carriers in the healthcare industry, for instance, in several applications, with drug delivery being among the most significant. These nanomaterials are adaptable and have qualities that are good for delivering compounds that are biologically active. The creation of different nanoparticles as a drug delivery system has led to the development of a variety of nanoparticulate drug delivery systems to reduce toxicity, reduce the dosing system, and increase the viability of the drug. The objectives of this review are to provide an overview of the recent advances in nanotechnology in Antifungal treatment and to overcome the problems associated with antifungal agents.

Background: Bioavailability is the dissimilarity between the total amount of drug exposure to a person and the actual dose received by his body. The difference in bioavailability between formulations of a given drug can have clinical implications. Methods: Poor aqueous solubility, inappropriate partition coefficient, high first-pass metabolism, narrow absorption window, and acidic pH of the stomach are the main reasons behind the low bioavailability of drugs. There are three substantial methods to vanquish these bioavailability issues, namely pharmacokinetic, biological, and pharmaceutical approaches. Results: In the pharmacokinetic approach a drug molecule is improved by making alterations in its chemical structure. In the biological approach, the course of administration of the drug is changed; for example, if a drug has very less oral bioavailability, it can be injected as parenteral or some other route if feasible. In the pharmaceutical approach to enhance bioavailability, the physiochemical properties of the drug or formulation are modified. It is cost-effective, less time-consuming, and the risk factor is also minimum. Co-solvency, particle size reduction, hydrotrophy, solid dispersion, micellar solubilisation, complexation, and colloidal drug delivery systems are some of the commonly used methods to enhance the dissolution profiles of drugs via the pharmaceutical approach. Similar to liposomes, niosomes are also vesicular carrier systems but non-ionic surfactants are used instead of phospholipids in their formulation, i.e., their bilayer is comprised of non-ionic surfactants that encircle the aqueous compartment. The niosomes are presumed to raise the bioavailability of poorly water-soluble drugs by increasing their uptake by the M cells present in Peyer's patches of lymphatic tissues of the intestine. Conclusion: Niosomal technology has become an attractive method to overcome several limitations due to its various merits like biodegradability, high stability, non-immunogenic nature, low cost, and flexibility to incorporate lipophilic as well as hydrophilic drugs. The bioavailability of many BCS class II and IV drugs has been successfully enhanced using niosomal technology, like Griseofulvin, Paclitaxel, Candesartan Cilexetil, Carvedilol, Clarithromycin, Telmisartan, and Glimepiride. Niosomal technology has also been exploited for brain targeting via nasal delivery for many drugs like Nefopam, Pentamidine, Ondansetron HCl, and Bromocriptine mesylate. Based on this data, it can be concluded that niosomal technology has increased importance in bioavailability enhancement and improving the overall performance of molecules in vitro and in vivo. Thus, niosomal technology holds tremendous potential for scale-up applications, overcoming the drawbacks of conventional dosage forms.

Background: Synthesizing a green source that has antimicrobial activity in nanoparticles is a novel and exciting approach to pharmaceutical science with promising results. Objective: Green-silver nanoparticles (G-AgNPs) were evaluated for their antimicrobial action on drugresistant pathogens. Methods: Lemon, black seeds, and flax were selected as green sources to synthesize nanoparticles formed with silver. Physical and chemical characteristics of these preparations were identified. The antimicrobial activities of the prepared compounds against drug-resistant clinical isolates of seven bacteria and five fungi were identified by disk diffusion and dilution methods. Results: The nanoparticle characteristics were confirmed by physical and chemical measurements. Lemon extract with silver nanoparticles (L-AgNP) showed more antimicrobial action, particularly on Gram-positive bacteria and Candida albicans. Silver nanoparticles with black seeds (B-AgNP) and flax (F-AgNP) had only antibacterial effects on a single bacterium (Enterobacter cloacae). Escherichia coli, Staphylococcus aureus, and two fungi, Candida glabrata and Candida utilis, showed resistance to all nanoparticles from plants. Conclusion: Lemon with silver nanoparticle is an effective plant product for use against various drugresistant species of human pathogens. Further pharmaceutical studies are required to verify the suitability of this form of the drug for human use. Another plant is recommended for testing against the most resistant strains of pathogens

Background: Ketoconazole is an imidazole ring containing antifungal agent used in the treatment of systemic fungal infections. It acts by blocking the synthesis of ergosterol, an essential component of the fungal cell membrane. Objective: The purpose of this work is to construct skin targeting ketoconazole nanostructured lipid carriers (NLCs) loaded hyaluronic acid (HA) modified gel to minimize side effects and provide a controlled release. Methods: The NLCs were prepared using emulsion sonication method and their optimized batches were characterized for X-ray diffraction, scanning electron microscopy and fourier transform infrared spectroscopy study. These batches were then incorporated into HA containing gel for convenient application. The final formulation was compared with the marketed formulation for studying its antifungal activity and drug diffusion. Results: Ketoconazole NLCs loaded hyaluronic acid formulation was successfully developed with desirable formulation parameters by using 23 Factorial design. In vitro release study of developed formulation showed prolonged drug release (up to 5 hrs) while ex vivo drug diffusion study on human cadaver skin showed better drug diffusion as compared with marketed formulation. Moreover, the release study and diffusion study results reflected the improvement of antifungal activity of the developed formulation against Candida albicans. Conclusion: The work suggests that ketoconazole NLCs loaded HA modified gel provides prolonged release. The formulation also has good drug diffusion and antifungal activity and thus can act as a promising carrier for topical delivery of ketoconazole.

Objective: Aluminum phosphide (AlP) as an effective pesticide may contribute to oxidative stress and adversely influence sperm parameters. This study aimed to investigate the protective role of curcumin and nanocurcumin on oxidative damage in the testis of rats with AlP toxicity. Methods: A total of 42 adult male Wistar rats were equally randomized into the following study groups (n = 7): Control, Control+Curcumin, Control+Nanocurcumin, AlP, AlP+Curcumin, and AlP+Nanocurcumin. The testis tissue was used to investigate the levels of testicular malondialdehyde (MDA), total oxidant status (TOS), total antioxidant capacity (TAC), and reduced glutathione (GSH) as well as the Catalase (CAT) and superoxide dismutase (SOD) enzyme activity. Epididymal sperm was used to perform sperm analysis. Results: AlP administration led to a significant increase in MDA, and TOS levels and also markedly decreased the SOD activity and the levels of TAC and GSH in testis tissue (p <0.001). Moreover, the motility and viability of sperms were significantly reduced (p <0.001). Curcumin and Nanocurcumin co-administration with AlP remarkably decreased the MDA and TOS level (p <0.001) and significantly increased the GSH and TAC levels as well as the activity of SOD in AlP intoxicated groups (p<0.001). Our findings demonstrated that Nanocurcumin administration has significantly enhanced the sperm quality in AlP intoxicated rats as compared to the control group (p <0.001). Conclusion: According to the results of this study, Curcumin as a potential antioxidant could be an effective attenuative agent against AlP-induced oxidative damage in testis, especially when it is used in encapsulated form, nanocurcumin.

Aims: This study aimed to prepare and evaluate the physicochemical and anticancer properties of cisplatin and curcumin-loaded mesoporous silica nanoparticles (Cis-Cur-MSNs). Background: In recent years, combination treatment has attained better outcomes than monotherapy in oncology. Cis-Cur-MSNs were prepared by precipitation technique. Objective: The objective of the present study was the evaluation of the physicochemical and anticancer properties of cisplatin and curcumin-loaded mesoporous silica nanoparticles (Cis-Cur-MSNs). Methods: The prepared materials were assessed in terms of physicochemical methods. The drug release pattern from the MSNs was also evaluated via ultraviolet spectrophotometry. In addition, the porosity and surface area of prepared nanoparticles were determined using the Brunauer-Emmett-Teller (BET) technique. The cytotoxicity of Cis-Cur-MSNs was evaluated on the HN5 cells as head and neck squamous carcinoma cell lines. Furthermore, ROS production of Cis-Cur-MSNs treated cells was evaluated compared with untreated cells. Results: According to the results, prepared nanoparticles displayed nanometer size, rod morphology, and negative surface charge with mesoporous structure belonging to the MCM-41 family (twodimensional hexagonal). Regarding the results of BET adsorption and desorption isotherm analysis for Cis-Cur-MSNs and drug-free MSNs, pore diameter, pore volume, specific surface area, and drug-loaded pore area in MSNs were decreased. In the first 10 days, the prepared nanoparticles exhibited a relatively rapid release pattern for cisplatin and curcumin, and until the 35th day, the release of them from the MSNs continued slowly. Conclusion: The cytotoxic effect of Cis-Cur-MSNs was significantly more than Cur-MSNs and Cis- MSNs in 24 and 48 h incubation time (p < 0.05). The results suggest that Cis-Cur-MSNs may be beneficial in the development of a cancer treatment protocol. Others: The prepared nanoparticle in the present study could be a potential biomaterial for cancer treatment.

Background: A drug with poor water-solubility, like Dexamethasone acetate, can present lower bioavailability conventional for pharmaceutical formulations, and the presence of polymorphs in the raw material can lead to drug quality problems. Objective: In this study, nanocrystals of dexamethasone acetate were synthesized by high pressure homogenizer (HPH) method in surfactant poloxamer 188 (P188) solid dispersion and the bioavailable in raw material with polymorphism presence was evaluated. Methods: The powder pre-suspension was prepared by the HPH process, and the nanoparticles formed were incorporated in P188 solutions. The nanocrystals formed were characterized by techniques of XRD, SEM, FTIR, thermal analysis by differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA), dynamic light scattering (DLS) to analyze the particle size and zeta potential, and in vitro evaluation by dissolution studies. Results: The characterization techniques were adequate to show the presence of raw material with physical moisture between two dexamethasone acetate polymorphs. The nanocrystals formed in the presence of the P188 in the formulation showed a considerable increase in the rate of dissolution of the drug in the medium and in the size of the stable nanocrystals, even in the presence of dexamethasone acetate polymorphs. Conclusion: The results showed that it was possible to produce dexamethasone nanocrystals by HPH process with regular size by the presence of the small amount of P188 surfactant. This article presents a novelty in the development of dexamethasone nanoparticles that have different polymorphic forms in their physical composition.

Introduction: Titanium-based implants are widely used due to their good biocompatibility and high corrosion resistance. Infections after implant placement are the main reason for the failure of implant treatment. Some recent studies have also shown that microbial contamination can occur at the implant-abutment level in implants with healthy or diseased surrounding tissue. The purpose of this study is to investigate the antibacterial effect of slow-release nanoparticles of polylactic co-glycolic acid (PLGA) loaded with chlorhexidine (CHX) inside the implant fixture. Materials and Methods: Thirty-six implants in three groups were examined in the bacterial culture environment. In the first group, PLGA/CHX nanoparticles; in the second group, the negative control group (distilled water) and in the third group, the positive control groups (chlorhexidine) were used. The bacterial suspensions, including Escherichia coli ATCC: 25922, Staphylococcus aureus ATCC: 6538 and Enterococcus faecalis ATCC: 29212 were used to investigate the antimicrobial effect of the prepared nanoparticles. Results: The results showed that the use of PLGA/CHX nanoparticles significantly inhibited the growth of all three bacteria. Nanoparticles loaded with chlorhexidine had a significant decrease in the growth rate of all three bacteria compared to chlorhexidine and water. The lowest bacterial growth rate was observed in the Enterococcus faecalis/PLGA nanoparticles group, and the highest bacterial growth rate was observed in the Staphylococcus aureus/H2O group. Conclusion: The current study showed that the use of PLGA/CHX nanoparticles could significantly inhibit the growth of all three bacteria. Of course, the current study was conducted in vitro, and to obtain clinical results, we need to conduct a study on human samples. In addition, the results of this study showed that the chemical antimicrobial materials could be used in low concentrations and in a sustained- released manner in cases of dealing with bacterial infections, which can lead to better and targeted performance as well as reduce possible side effects.

Introduction: For the long-term success of implant treatment, prevention of biological complications, including pre-implant diseases, plays an important role. The use of antimicrobial coatings is one of the prosperous methods in this field. The aim of this study is to evaluate the antimicrobial effects of healing abutments coated with gelatin-curcumin nanocomposite. Methods: This study included 48 healing abutments in the form of a control group (titanium healing abutments without coating) and an intervention group (titanium healing abutments coated with gelatincurcumin nanocomposite). The disc diffusion method was used to evaluate the antimicrobial effects of coated healing abutments against Escherichia coli, Staphylococcus aureus and Enterococcus faecalis and the results were reported in a non-growth zone area. Results and Discussion: Gelatin-curcumin nanocomposite caused significant non-growth aura for all three bacteria compared to the control group. For the control group (healing abutments without coating), the antimicrobial effects (non-growth zone) were zero. Besides, gelatin-curcumin nanocomposite had the greatest inhibiting effect on the growth of S. aureus, then E. coli and finally E. faecalis. Conclusion: The results of our study showed that the coating used was able to significantly demonstrate a non-growth zone against all three bacteria compared to the control group without coating. Further evaluations in various physicochemical, mechanical, and antimicrobial fields are necessary for the animal model and clinical phase.