Development and In Vitro Characterization of Antibiotic-Loaded Nanocarriers for Dental Delivery.

The aim of this research work was to formulate and evaluate ciprofloxacin hydrochloride-loaded nanocarriers for treating dental infections and bone regeneration. Periodontal infection is associated with inflammation, soft tissue destruction, and bone loss. The objective of the study was to extract ß tricalcium phosphate (ß-TCP) from coral beach sand using the hydrothermal conversion method and load these nanocarriers with ciprofloxacin hydrochloride. The developed drug-loaded nanocarriers were evaluated for various parameters. In vitro drug-loading studies showed the highest drug loading of 71% for F1 with a drug: carrier ratio compared to plain ciprofloxacin hydrochloride gel. ß-TCP and nanocarriers were evaluated for powder characteristics and the results were found to have excellent and fair flowability. In vitro drug release studies conducted over a period of 5 days confirmed the percentage drug release of 96% at the end of 120 h. Nanocarriers were found to be effective against S. aureus and E. coli showing statistically significant antibacterial activity at (* p < 0.05) significant level as compared to plain ciprofloxacin hydrochloride gel. The particle size of ß-TCP and nanocarriers was found to be 2 µm. Fourier transform infra-red studies showed good compatibility between the drug and the excipients. Differential scanning calorimetry studies revealed the amorphous nature of the nanocarriers as evident from the peak shift. It is obvious from the XRD studies that the phase intensity was reduced, which demonstrates a decrease in crystallinity. Nanocarriers released the drug in a controlled manner, hence may prove to be a better option to treat dental caries as compared to conventional treatments.

Formulation, Characterization, and Evaluation of Eudragit-Coated Saxagliptin Nanoparticles Using 3 Factorial Design Modules.

Background and Introduction: Saxagliptin is a hypoglycemic drug that acts as a dipeptidyl peptidase-4 (DPP-4) inhibitor and is preferably used in the treatment of Type 2 Diabetes Mellitus (T2DM). It is safe and tolerable; however, the major disadvantage associated with it is its low bioavailability. Aim: The present research aimed to enhance the bioavailability of the drug by enteric coating with a polymer that controls the rate of drug delivery, and it was prepared as Solid Lipid Nanoparticles (SLNs). Methodology: In the current study, various SLN formulations were developed using a central composite design (CCD) module using Design Expert-11 software. A modified solvent injection technique was used to prepare Saxagliptin nanoparticles coated with Eudragit RS100. The CCD was used to determine the independent variables and their effect on dependent variables at varied levels. Evaluation studies such as particle size analysis, Zeta potential, polydispersity index (PDI), drug loading, entrapment efficiency, in-vitro drug release studies, and in vivo pharmacokinetic studies were performed for the optimized SLN formulation. The reversed-phase HPLC method was developed and validated for the estimation of the pharmacokinetic parameters of the pure drug and prepared SLNs. Results: The effect of independent variables (A1: amount of lipid, A2: amount of polymer, A3: surfactant concentration, and A4: homogenization speed) on dependent variables (R1: particle size, and R2: entrapment efficiency) was established in great detail. Observed responses of the prepared and optimized Saxagliptin SLN were close to the predicted values by the CCD. The prepared SLNs depicted particle sizes in the range of 212-442 nm. The particle size analysis results showed that an increase in the lipid concentration led to an increase in particle size. The developed bioanalytical method was noted to be very specific and robust. The method accuracy varied from 99.16% to 101.95% for intraday, and 96.08% to 103.12% for inter day operation at low (5 mcg/mL), moderate (10 mcg/mL), and higher (15 mcg/mL) drug concentrations. The observed Zeta potential values for the prepared SLNs were in the range of -41.09 ± 0.11 to 30.86 ± 0.63 mV suggesting quite good stability of the SLNs without any aggregation. Moreover, the polydispersity indices were in the range of 0.26 ± 0.051 to 0.45 ± 0.017, indicative of uniformity of sizes among the prepared SLNs. In vivo study outcomes proved that Saxagliptin oral bioavailability significantly enhanced in male Albino Wistar Rats via SLN formulation and Eudragit RS100 coating approach. Conclusions: The developed and optimized Saxagliptin SLNs revealed enhanced Saxagliptin bioavailability in comparison to the native drug. Thus, this formulation strategy can be of great importance and can be implied as a promising approach to enhance the Saxagliptin bioavailability for facilitated T2DM therapy.

Smart Nanocarriers as an Emerging Platform for Cancer Therapy: A Review.

Cancer is a group of disorders characterized by uncontrolled cell growth that affects around 11 million people each year globally. Nanocarrier-based systems are extensively used in cancer imaging, diagnostics as well as therapeutics; owing to their promising features and potential to augment therapeutic efficacy. The focal point of research remains to develop new-fangled smart nanocarriers that can selectively respond to cancer-specific conditions and deliver medications to target cells efficiently. Nanocarriers deliver loaded therapeutic cargos to the tumour site either in a passive or active mode, with the least drug elimination from the drug delivery systems. This review chiefly focuses on current advances allied to smart nanocarriers such as dendrimers, liposomes, mesoporous silica nanoparticles, quantum dots, micelles, superparamagnetic iron-oxide nanoparticles, gold nanoparticles and carbon nanotubes, to list a few. Exhaustive discussion on crucial topics like drug targeting, surface decorated smart-nanocarriers and stimuli-responsive cancer nanotherapeutics responding to temperature, enzyme, pH and redox stimuli have been covered.

Development and in vitro evaluation of effervescent floating matrix tablet of neritinib: An anticancer drug.

Neratinib is a potent anticancer drug, used for the treatment of breast cancer. It is poorly soluble at higher pH, which tends to minimize the therapeutic effects in the lower GIT leads to its poor bioavailability. An attempt has been made to prepare and develop a novel gastro-retentive system of neratinib to improve the drug bioavailability in the GIT by enhancing the gastric retention time. The floating matrix tablets were prepared by various proportions of carbopol 940, micro-crystalline cellulose (MCC) and ethyl cellulose (EC), sodium bicarbonate (NaHCO3) as gas forming agent, by direct compression. The formulation mixture was assessed for pre and post compression test, lag time, in-vitro floating, FTIR, water uptake/swelling index, in vitro and kinetic release studies. The findings revealed that, the parameters of compression (pre and post) were within USP limits. The floating tablets swelled well and floated for more than 24h, with less than 120 seconds of buoyancy lag time. The optimized formulation F3 showed sustained release up to 12h; a non-Fickian mechanism. Therefore, all the results and findings have shown that developed neratinib floating matrix system is a promising approach as a drug delivery system and application in the treatment of breast cancer.

Characterization, Optimization, In Vitro and In Vivo Evaluation of Simvastatin Proliposomes, as a Drug Delivery.

Simvastatin a cholesterol-lowering agent used to treat hypercholesterolemia, coronary heart disease, and dyslipidemia. However, simvastatin (SV) has shown low oral bioavailability in GIT. The main purpose of the work was to develop proliposomal formulations to increase the oral bioavailability of SV. Film deposition on the carrier method has been used to prepare the proliposomes. The proliposomes were assessed for morphology, particulate size, entrapment efficacy, drug-polymer compatibility, in vitro and in vivo studies. FTIR and DSC results revealed no drug-polymer interaction. SEM and XRD analysis conform; proliposomes are spherical, amorphous in nature, so that it enhances the solubility of SV between 15.01 ± 0.026 and 57.80 ± 0.015 µg/mL in pH 7.4 phosphate buffer. The optimised formulation (PL6) shows drug release up to 12 h (99.78 ± 0.067%). The pharmacokinetics of pure SV and SV proliposomes (SVP) in rats were Tmax 2 ± 0.5 and 4 ± 0.7 h, Cmax 10.4 ± 2.921 and 21.18 ± 12.321 µg/mL, AUC0-∞ 67.124 ± 0.23 and 179.75 ± 1.541 µg/mL h, respectively. Optimised SVP shows a significant improvement in the rate and absorption of SV. The optimised formulation showed enhanced oral bioavailability of SV in Albino Wister rats and offers a new technique to improve the poor water-soluble drug absorption in the gastrointestinal system.

Pioneering a paradigm shift in tissue engineering and regeneration with polysaccharides and proteins-based scaffolds: A comprehensive review.

In the realm of modern medicine, tissue engineering and regeneration stands as a beacon of hope, offering the promise of restoring form and function to damaged or diseased organs and tissues. Central to this revolutionary field are biological macromolecules-nature's own blueprints for regeneration. The growing interest in bio-derived macromolecules and their composites is driven by their environmentally friendly qualities, renewable nature, minimal carbon footprint, and widespread availability in our ecosystem. Capitalizing on these unique attributes, specific composites can be tailored and enhanced for potential utilization in the realm of tissue engineering (TE). This review predominantly concentrates on the present research trends involving TE scaffolds constructed from polysaccharides, proteins and glycosaminoglycans. It provides an overview of the prerequisites, production methods, and TE applications associated with a range of biological macromolecules. Furthermore, it tackles the challenges and opportunities arising from the adoption of these biomaterials in the field of TE. This review also presents a novel perspective on the development of functional biomaterials with broad applicability across various biomedical applications.

Drug eluting protein and polysaccharides-based biofunctionalized fabric textiles- pioneering a new frontier in tissue engineering: An extensive review.

In the ever-evolving landscape of tissue engineering, medicated biotextiles have emerged as a game-changer. These remarkable textiles have garnered significant attention for their ability to craft tissue scaffolds that closely mimic the properties of natural tissues. This comprehensive review delves into the realm of medicated protein and polysaccharide-based biotextiles, exploring a diverse array of fabric materials. We unravel the intricate web of fabrication methods, ranging from weft/warp knitting to plain/stain weaving and braiding, each lending its unique touch to the world of biotextiles creation. Fibre production techniques, such as melt spinning, wet/gel spinning, and multicomponent spinning, are demystified to shed light on the magic behind these ground-breaking textiles. The biotextiles thus crafted exhibit exceptional physical and chemical properties that hold immense promise in the field of tissue engineering (TE). Our review underscores the myriad applications of drug-eluting protein and polysaccharide-based textiles, including TE, tissue repair, regeneration, and wound healing. Additionally, we delve into commercially available products that harness the potential of medicated biotextiles, paving the way for a brighter future in healthcare and regenerative medicine. Step into the world of innovation with medicated biotextiles-where science meets the art of healing.

Unravelling the in vivo dynamics of liposomes: Insights into biodistribution and cellular membrane interactions.

Liposomes, as a colloidal drug delivery system dating back to the 1960s, remain a focal point of extensive research and stand as a highly efficient drug delivery method. The amalgamation of technological and biological advancements has propelled their evolution, elevating them to their current status. The key attributes of biodegradability and biocompatibility have been instrumental in driving substantial progress in liposome development. Demonstrating a remarkable ability to surmount barriers in drug absorption, enhance stability, and achieve targeted distribution within the body, liposomes have become pivotal in pharmaceutical research. In this comprehensive review, we delve into the intricate details of liposomal drug delivery systems, focusing specifically on their pharmacokinetics and cell membrane interactions via fusion, lipid exchange, endocytosis etc. Emphasizing the nuanced impact of various liposomal characteristics, we explore factors such as lipid composition, particle size, surface modifications, charge, dosage, and administration routes. By dissecting the multifaceted interactions between liposomes and biological barriers, including the reticuloendothelial system (RES), opsonization, enhanced permeability and retention (EPR) effect, ATP-binding cassette (ABC) phenomenon, and Complement Activation-Related Pseudoallergy (CARPA) effect, we provide a deeper understanding of liposomal behaviour in vivo. Furthermore, this review addresses the intricate challenges associated with translating liposomal technology into practical applications, offering insights into overcoming these hurdles. Additionally, we provide a comprehensive analysis of the clinical adoption and patent landscape of liposomes across diverse biomedical domains, shedding light on their potential implications for future research and therapeutic developments.

Advancements in gelatin-based hydrogel systems for biomedical applications: A state-of-the-art review.

A gelatin-based hydrogel system is a stimulus-responsive, biocompatible, and biodegradable polymeric system with solid-like rheology that entangles moisture in its porous network that gradually protrudes to assemble a hierarchical crosslinked arrangement. The hydrolysis of collagen directs gelatin construction, which retains arginyl glycyl aspartic acid and matrix metalloproteinase-sensitive degeneration sites, further confining access to chemicals entangled within the gel (e.g., cell encapsulation), modulating the release of encapsulated payloads and providing mechanical signals to the adjoining cells. The utilization of various types of functional tunable biopolymers as scaffold materials in hydrogels has become highly attractive due to their higher porosity and mechanical ability; thus, higher loading of proteins, peptides, therapeutic molecules, etc., can be further modulated. Furthermore, a stimulus-mediated gelatin-based hydrogel with an impaired concentration of gellan demonstrated great shear thinning and self-recovering characteristics in biomedical and tissue engineering applications. Therefore, this contemporary review presents a concise version of the gelatin-based hydrogel as a conceivable biomaterial for various biomedical applications. In addition, the article has recapped the multiple sources of gelatin and their structural characteristics concerning stimulating hydrogel development and delivery approaches of therapeutic molecules (e.g., proteins, peptides, genes, drugs, etc.), existing challenges, and overcoming designs, particularly from drug delivery perspectives.

Conductive polymers and composites-based systems: An incipient stride in drug delivery and therapeutics realm.

Novel therapies and drug delivery systems (DDS) emphasis on localized, personalized, triggered, and regulated drug administration have heavily implicated electrically responsive DDS. An ideal DDS must deliver drugs to the target region at therapeutically effective concentrations to elicit a pharmacological response, resulting in better prophylaxis of the disease and the treatment. Biodegradable polymers are frequently employed for in-vivo long-term release; however, dose dumping can be anticipated. As a result, current DDSs can be tagged as dubbed "Smart Biomaterials" since they only focus on an on-demand cargo release in response to a trigger or stimulation. These organic materials have been recognized for their metal-like conductivity, as well as their mechanical stability and ease of production. These biomaterials can be programmed to respond to both internal and external stimuli. External pulsed triggers are required for extrinsic stimuli-responsive materials, whereas intrinsic stimuli-responsive materials rely on localized changes in the tissue environment. Furthermore, these materials have the ability to deliver active pharmaceutical agents at a varied concentration levels and across a broad spectrum of action. Drug delivery, biomedical implant technology, biosensor technology, and tissue engineering can be listed as a few prominent applications that have sparked immense interest for conductive polymers-based research and advancements in academia as well as in industry. This review comprehensively covers a cutting-edge collection of electrically conductive polymers and composites, and provide detailed insights of recent trends and advancements allied to conductive polymers for their potential applicability in an array of diverse meadows primarily focusing on drug delivery, biosensing and therapeutics. Furthermore, progressions in their synthesis, structural and functional properties have been presented in conjunction with futuristic directions for the smooth clinical translations.

Development of stealth liposomal formulation of celecoxib: In vitro and in vivo evaluation.

Celecoxib (CLB) is a highly hydrophobic selective cyclo-oxygenase inhibitor with high plasma protein binding and undergoes extensive hepatic metabolism. CLB is highly effective in the treatment of osteo and rheumatoid arthritis as first line therapy but produces severe gastro-intestinal toxicities and cardiovascular side effects. In this research, stealth liposomes of CLB were developed with the intention to reduce the side effects and increase the accumulation of drug in the sites of inflammation. Stealth liposomes were prepared by thin film hydration technique using distearoylphosphatidylcholine and PE-PEG 2000 with variable amounts of cholesterol and characterized. The effects of various lipids such as hydrogenated soy phosphatidylcholine, dipalmitoyl phosphatidylcholine, distearoylphosphatidylcholine and cholesterol content on % drug encapsulation was investigated. The optimized stealth liposomes were characterized by FT-IR and DSC for possible drug excipients interaction. Pharmacokinetics, pharmacodynamics and biodistribution studies were carried out for the stealth liposomes. The results revealed that the stealth liposomes reduced the inflammation to the larger magnitude and have also sustained the magnitude when compared to free drug along with maximum analgesic response. Higher elimination half-life, AUC, MRT and lowered clearance rate denotes the extended bioavailability of the drug in blood. Biodistribution studies revealed that stealth liposomes extend the circulation time of liposomes in blood by decreasing opsonisation and be less concentrated in kidney, thereby reducing the toxicities to RES and renal organs and facilitate the drug accumulation in the area of inflammation. Our results indicated that CLB, without the requirement of modifications to enhance solubilisation, can be encapsulated and released from liposomal formulations. This new-fangled drug delivery approach may be used to circumvent the low bioavailability and toxic side effects of oral CLB formulations.

A novel RP-HPLC method development and validation for simultaneous quantification of gefitinib and resveratrol in polymeric hybrid lipid nanoparticles and glioma cells.

Resveratrol and Gefitinib are adjunct therapies for various cancers; however, both have been limited by low solubility, low cellular uptake, and bioavailability issues. As a result, this research aimed to develop an accurate, precise, selective, and sensitive reverse-phase high-performance liquid chromatography (RP-HPLC) method to simultaneously determine both compounds in nanoformulation and Glioma cells. The phenomenex luna C8 column, a mobile phase (80: 20 ratios of acetonitrile: 200 mM ammonium acetate) with a flow rate of 1 mL. min-1, 40 ± 0.2 °C as a column temperature, and the injection volume was 20 µl were selected as optimized chromatographic conditions. Retention time (RT) of resveratrol (1.80 min) and gefitinib (2.56 min) were identified using an optimized analytical method and detected at 345 nm (isosbestic point). The approach was proven to be specific for resveratrol and gefitinib analysis in the existence of PHLNPs, precise (RSD 2 %), and accurate (>90 %). The simultaneous analytical method was successfully developed to identify percentage drug entrapment efficiency (% DEE), % drug loading (% DL) of resveratrol and gefitinib in PHLNPs, and secondary estimates of in-vitro drug release profile and percentage cellular uptake studies. The in-vitro results revealed that the developed analytical method could simultaneously detect and quantify these drugs in other nanoformulations and in-vivo studies.

Pharmacological Efficacy of Tamarix aphylla: A Comprehensive Review.

Tamarix aphylla is a well-known species of the genus Tamarix. T. aphylla (Tamaricaceae) is a perennial tree in Asia, the Middle East, and Central Africa. It is used as a carminative diuretic in tuberculosis, leprosy, and hepatitis. Various pharmacological properties have been shown by T. aphylla, such as antidiabetic, anti-inflammatory, antibacterial, antifungal, anticholinesterase, and wound-healing activity. However, T. aphylla has not received much attention for its secondary metabolites and bioactive constituents. Research has shown that this plant has hidden potential that needs to be explored. This review aims to cover botanical classification, geographical distribution, taxonomy, ethnobotanical uses, and the phytochemical compounds found in T. aphylla. The toxicology and pharmacological effects of T. aphylla are also discussed. We examined various scholarly resources to gather information on T. aphylla, including Google Scholar, Scopus, Science Direct, Springer Link, PubMed, and Web of Science. The finding of this work validates a connection between T. aphylla in conventional medicine and its antidiabetic, antibacterial, anti-inflammatory, wound-healing, antifungal, anticholinesterase, and other biological effects. T. aphylla's entire plant (such as bark, leaves, fruits) and root extracts have been used to treat hypertension, stomach discomfort, hair loss, cough and asthma, abscesses, wounds, rheumatism, jaundice, fever, tuberculosis, and gum and tooth infection. The phytochemical screening revealed that noticeably all extracts were devoid of alkaloids, followed by the presence of tannins. In addition, different parts have revealed the existence of steroids, flavonoids, cardiac glycosides, and byproducts of gallic acid and ellagic acid. T. aphylla has shown many valuable activities against different diseases and supports its traditional uses. Therefore, high-quality preclinical research and well-designated clinical trials are needed to establish the efficacy and safety of this plant in humans.

Nanosponge Carriers- An Archetype Swing in Cancer Therapy: A Comprehensive Review.

Nanotechnology and nanomedicines are emerging research meadows; which chiefly focuses on creating and manipulating materials at a nanometer level for the betterment in imaging, diagnosis and treatment of a range of diseases together with cancer. Cyclodextrin-based nanosponges, anticipated as a new-fangled nanosized delivery system, are ground-breaking hyper-crosslinked cyclodextrin polymers nanostructured within a three-dimensional network. Nanosponges based systems hold the potential of elevating the solubility, absorption, penetration, bioavailability, in vivo stability, targeted as well as sustained delivery, and therapeutic efficiency of numerous anticancer agents. The extension of nanosponges based drug delivery systems is an exhilarating and demanding research pasture, predominantly to overcome aforementioned problems allied to existing anticancer formulations and for the further progressions in cancer therapies. Nanosponges in cancer therapy, particularly cyclodextrin based nanosponges are brought up in this review. By quoting diverse attempts made in pertinent direction, efforts have been made to exemplify the characteristics, suitability and versatility of cyclodextrin based nanosponges for their promising applications in cancer treatment.

Current Perspectives on Novel Drug Delivery Systems and Therapies for Management of Prostate Cancer: An Inclusive Review.

BACKGROUND: Prostate cancer (PC) is a prostate gland cells carcinoma, the foremost reason of cancer deaths in men in developed countries, representing most common malignancy in adult males. The key obstacle to achieve practicable therapeutic effect of active drugs and capable hopeful agents including proteins and peptides, and nucleic acid for prostate cancer is the scarcity of targeted drug delivery to cells of prostate cancer. As a result, need for novel systems, strategies or therapeutic approaches to enhance the assortment of active agents meant for prostate cancer becomes an important criterion. Currently cancer research focuses on improving treatment of prostate cancer using various novel drug delivery systems of chemotherapeutic agents. These novel drug delivery systems comprise nanoparticles and liposomes. Also, strategies or therapeutic approaches intended for the prostate cancer include radiation therapy for localized prostate cancer, hormonal therapy for suppressing tumor growth, and gene-and-immunologic therapy. These systems and approaches can deliver the drugs to their selected or targeted cancer cells for the drug release in cancer atmosphere of prostate thereby enhancing the effectiveness of tumor penetration. OBJECTIVE: The objective was to collect and report the recent research findings to manage the PC. Present review encloses existing diverse novel drug delivery systems and approaches intended for the management of PC. CONCLUSION: The reported miscellaneous novel drug delivery systems along with the diverse therapies are seem to be precise, secure and relatively effective; and in consequence could lead to a new track for obliteration of prostate cancer.