Vol 14, No 1 (2024)
- Year: 2024
- Articles: 8
- URL: https://cardiosomatics.ru/2468-1873/issue/view/12774
Pharmacology
The Versatility of Natural Excipient Zein Utilized in Nanocarriers for Improving Biopharmaceutical Attributes



A Recent Review on Nanocrystal Manufacturing Techniques with Pharmaceutical Application
Abstract
This review article constitutes an introductory report on nanotechnology focusing on the various manufacturing approaches of nanocrystals. Nanocrystals are a solid form to tackle the issue identified with poor fluid solvency. Hence, it is a useful technique in improving the bioa-vailability of various poorly soluble drugs. On a broader way, nanocrystal technology is mainly classified as top-down technology, bottom-up technology and a combination of top-down and bottom-up technology. Top-down technology is based on the principle of breaking down a com-plex into small crystals. This process is executed by using high-pressure homogenization, laser ablation, media mills, ultrasound technology, vacuum dissolution, gas condensation and mechani-cal attrition. Bottom-up technology is based on the principle of preparation by gathering at-oms/molecules together. It is achieved by using precipitation, supercritical fluid, gel-gel technol-ogy, spray drying, hydrolysis, and condensation. Due to the diverse characteristics and properties of drugs, a combination of top-down and bottom-up techniques is best for manufacturing nano-crystals. Some of the promising technique includes nano-edge technology and smart-crystal tech-nology. These techniques are discussed in this review.



Chitosan-based Nanomedicine in the Management of Age-related Macular Degeneration: A Review
Abstract
Age-related macular degeneration (AMD) is a leading cause of permanent blindness globally. Due to the various obstacles, highly invasive intravitreal (IVT) injections are the prima-ry method used to deliver medications to the tissues of the posterior eye. An utmost patient-friendly topical ocular delivery approach has been extensively researched in recent years. Muco-adhesive compositions extend precorneal residence time while reducing precorneal clearance. They increase the likelihood of adhesion to corneal and conjunctival surfaces and, as a result, al-low for enhanced delivery to the posterior eye segment. Due to its remarkable mucoadhesive characteristics, chitosan (CS) has undergone the most extensive research of any mucoadhesive polymer. Drug delivery to the front and back of the eye is still difficult. The pharmaceutical in-dustry has shown greater interest in drug delivery systems (DDSs) based on nanotechnology (NT) in recent years, particularly those made from natural polymers like chitosan, alginate, etc. Be-cause of their incredible adaptability, higher biological effects, and favourable physicochemical properties, CS-oriented nanomaterials (NMs) are explored by researchers as prospective nanocar-riers. CS are the right substrates to develop pharmaceutical products, such as hydrogels, nanopar-ticles (NP), microparticles, and nanofibers, whether used alone or in composite form. CS-based nanocarriers deliver medicine, such as peptides, growth factors, vaccines, and genetic materials in regulated and targeted form. This review highlights current developments and challenges in chi-tosan-mediated nano therapies associated with AMD.



Formulation of Lipid Nanoparticles based Nanogel of Sertaconazole Nitrate and its Evaluation
Abstract
Background:Sertaconazole nitrate is a topical antifungal drug used to treat interdigital tinea pedis in patients with immunocompetent conditions. The class of imidazole includes the antifungal medication sertaconazole nitrate. It is available in topical formulations for treating skin infections, including athlete's foot. Solid lipid nanoparticles (SLN) are at the cutting edge of nanotechnology, with several potential uses in drug delivery and research. Because of their unique size-dependent features, lipid nanoparticles hold the promise of novel therapies.
Objective:Drug incorporation into nanocarriers creates a new drug delivery prototype that could be employed for drug targeting. The research aims to study the formulation and evaluation of Sertaconazole nitrate solid lipid nanoparticles. The goal behind formulating SLN gel is to provide and maintain therapeutic concentrations of the drug at the target biological site to maximise therapeutic efficacy and minimise side effects.
Methods:Sertaconazole Nitrate Solid Lipid Nanoparticles are prepared by using High Pressure Homogenizer to get nanogel formulation as the final formulation and In-vitro drug release using a diffusion apparatus. The prepared SLNs were evaluated in their FTIR studies to determine compatibility between the drug and the excipients; zeta potential indicates the solid lipid nanoparticle was stable, and polydispersity index was used to determine particle size.
Result:The results demonstrate that optimised SLN-based Sertaconazole nitrate gel exhibited the best physicochemical properties, including FTIR studies of the drug, excipients, and optimised formulation demonstrate that all are compatible with each other, particle size is less than 200 nm, zeta potential ranging from 12 to -20 mV, and highest entrapment efficiency is 71.48%. Optimised solid lipid nanoparticles showed good in vitro release and antimicrobial results. The main application of SLN large scale-up is possible, and the drug can be effective with less dose incor-poration.
Conclusion:In this research work, the proposed plan of work SLN of Sertaconazole Nitrate was formulated successfully. The preliminary identification tests were performed, such as melting point determination, estimation of λmax by UV-visible spectrophotometry and plot of its calibration curve in solvent and buffer system, and FT-IR investigation to confirm the purity and confirmation of medication. High physical stability and drug loading are advantageous to SLN.



PEGylated Chitosan Biodegradable Nanoparticles Delivery of Salvia officinalis and Melissa officinalis for Enhanced Brain Targeting
Abstract
Background:Alzheimer's disease (AD) is a progressive neurodegenerative condition characterized by the gradual decline of cognitive abilities, primarily caused by impairments in the cholinergic system. AD is diagnosed based on the presence of specific pathological features, in-cluding senile plaques, neurofibrillary tangles, and the loss of neurons and synapses. Despite on-going efforts, the etiology of AD remains unclear, and there is a significant lack of effective treatments to meet the medical needs of affected individuals. The complex nature of AD, involv-ing multiple factors, presents challenges in the development of potential therapies. Numerous ob-stacles hinder the achievement of optimal pharmacological concentration of promising molecules for AD treatment. These obstacles include the presence of the blood-brain barrier (BBB), which restricts the entry of therapeutic agents into the brain, as well as issues related to poor bioavaila-bility and unfavorable pharmacokinetic profiles. Unfortunately, many therapeutically promising compounds have failed to overcome these hurdles and demonstrate efficacy in treating AD.
Methods:The PEGylated chitosan nanoconjugate was developed and evaluated for delivery of anti-Alzheimer natural extract of Salvia officinalis and Melissa officinalis to the brain. The nano-conjugates (S-PCN and M-PCN) were developed by ionic gelation technique.
Result:The nanoconjugates (S-PCN and M-PCN) were evaluated for various optical and in-vitro parameters. MTT assay on UCSD229i-SAD1-1 human astrocytoma cells indicated IC50 values of 0.42, 0.49, 0.67, and 0.75 µM for S-PCN, M-PCN formulations, and free Salvia officinalis and Melissa officinalis extracts, respectively. The In vitro assessments using cell lines have confirmed the improved uptake and distribution of nanoconjugates compared to free extracts. These findings were validated through confocal microscopy and apoptosis assays, revealing a substantial in-crease in the accumulation of nanoconjugates within the brain. The targeting potential OF M- PCN over S-PCN was found to be 2-fold significant.
Conclusion:Based on the findings, it can be inferred that biodegradable PEGylated chitosan nanoconjugates hold promise as effective nano-targeting agents for delivering anti-Alzheimer drugs to the brain. The incorporation of PEGylated chitosan nanoparticles in this approach demonstrates enhanced delivery capabilities, ultimately leading to improved therapeutic out-comes.



Development of In-situ Gel of Bupropion Hydrochloride-loaded Chitosan Nanoparticles using an Inotropic Gelation Method for Smoking Cessation via Nose to Brain: In-vitro and Ex-vivo Characterization and Evaluation
Abstract
Introduction:Tobacco use is the leading preventable cause of various diseases, disabili-ties, and death. It is estimated that 480000 deaths annually are attributed to cigarette smoking, in-cluding secondhand smoke exposure. The treatment of brain disorders is particularly challenging due to the presence of a variety of formidable obstacles to delivering drugs selectively and effec-tively to the brain. The blood-brain barrier (BBB) and first-pass metabolism constitute the major obstacle to the uptake of drugs into the brain following systemic administration. Intranasal delivery offers a non-invasive and convenient method to bypass the BBB and avoid first-pass metabolism, which leads to the delivery of therapeutics directly to the brain.
Objective:The objective of this study was to develop an In-situ gel of Bupropion Hydrochloride-loaded chitosan nanoparticles using the inotropic gelation method for Smoking Cessation via the nose to the brain to improve the bioavailability of Bupropion Hydrochloride, avoiding first-pass me-tabolism and bypassing Blood Brain Barrier.
Methods:Fourier transform infrared spectroscopy (FTIR) was used to determine the identity and purity of the drug. A UV Spectrophotometer was employed in the analytical procedure. Chitosan nanoparticles loaded with bupropion HCl were made using the ionic gelation method, and then the optimized batch was made using simulated in-situ gelation. Utilizing Central composite design, op-timization was done by Design Expert-13. Evaluation of polymeric nanoparticles was performed by measuring their particle size, PDI, and entrapment efficiency. Additionally, they were tested for drug release in vitro. The final nanoparticles were subsequently tested for gelation using nasal simulation fluid, and an ex vivo investigation was also conducted. An ion-sensitive polymer gellan gum was used as a gelling agent, which formed an immediate gel and remained for an extended period. The finished formulation was also subjected to several characteri-zations, including TEM and FTIR.
Results:The developed formulation was stable and showed enhanced contact time in the nasal mu-cosa, minimizing the frequency of administration. In-vitro studies through Franz diffusion cell and Ex-vivo studies on sheep nasal mucosa showed good results. In the Histopathological study, the op-timized batch was found to be safe and stable in an accelerated stability study for one month.
Conclusion:Bupropion HCl-loaded chitosan nanoparticles In-situ gel proved to be suitable for the administration of Bupropion HCl through the nasal route. The ease of administration coupled with less frequent administration enhanced patient compliance. The formulation was found to be liquid at the formulated condition and formed gel in the presence of ions present in the nasal mucosa. The gel formed in situ showed sustained drug release. The formulations were less viscous before instilla-tion and formed a strong gel after instilling in the nasal cavity.



Synthesis and Characterization of Copper Nanoparticles Using Plant Extract of Mentha piperita Leaves, Anethum graveolens L., and Calotropis procera
Abstract
Background:Synthesis of copper nanoparticles needs to be carried out with the use of environmentally safer alternatives. Plant-mediated nano-fabrication is a new area of nanotechnology that is favoured over traditional methods due to its effectiveness with respect to safety, affordability, environmental friendliness, and biocompatibility. Synthesis of copper nanoparticles using natural sources is the demand of this era.
Methods:In the present study, the synthesis of copper nanoparticles (CuNPs) was carried out us-ing three different plant extracts, i.e., Mentha piperita, Anethum graveolens L., and Calotropis procera. This synthesis was carried out in different conditions and the visual colour change in the solution confirmed the presence of copper nanoparticles. The nanoparticles were also character-ized with UV-vis absorption spectroscopy and scanning electron microscope (SEM).
Conclusion:In comparison to the synthetic route, the current work represents a cost-effective and sustainable way for the synthesis of nanoparticles.



Preparation and Evaluation of Nanoemulgel with Seed Oils for Skin Care
Abstract
Introduction:Skin is aging external organ protecting the entire body from a complicated process that affects all living things. Vegetable oils give the epidermis a barrier that shields it and halts water loss. Polyunsaturated fatty acids, phenolic and flavonoid content present in grape seed oil (GSO), papaya seed oil (PSO), and flaxseed oil (FSO) are reported for their antioxidant and moisturizing effect when applied as a topical formulation for skin care
Objective:In the present work, the oils were screened for their antioxidant activity and skin-whitening properties and formulated as nanoemulgel.
Methodology:The oils studied for their phenolic and flavonoid content and formulated as a nano emulgel using Tween 80 and Transcutol. Further, the formulation was evaluated for its physico-chemical properties and stability.
Results:The oils' total phenolic and flavonoid content was determined using gallic acid and rutin trihydrate, respectively as standards. The % oleic acid content was determined by using HPTLC where PSO had the highest oleic acid content (54.04%) as compared to GSO and FSO.
Conclusion:All oils exhibited significant antioxidant activity and tyrosinase enzyme inhibition due to the phenolic components, flavonoids, and tocopherols. Based on the phytoactive present, nanoemulsion in different proportions (3% oil mix and 5% oil mix in a ratio of 1:1:1 and 1.5:1.5:2 for GSO: PSO: FSO) was formulated. Globule size and PDI of the optimized nanoemulsion batch were obtained as 181 nm and 0.292, respectively. Further optimization of formulation and its efficacy and dermatokinetics can be studied.


