Drug Entrapment Efficiency Research Articles

Design and Characterization of Hallow Porous Floating Microspheres of Favipiravir

The present investigation deals with the design and characterization of favipiravir floating microspheres for gastro retentive drug delivery system by employing 3² factorial design and also to investigate the main effects of different independent variables on microspheres that float. The emulsion solvent diffusion method was used to manufacture floating microspheres with Eudragit S 100 as the polymer. These microspheres will extend the release of the medicine, reducing the frequency of administration and the harmful effects caused by fluctuations in plasma concentration with conventional dosage forms. The main effect of independent variables like polymer Eudragit S 100 concentrations (50, 100, 150 mg) and stirring time (1, 2 and 3 hours) on the performance of microspheres. Formulated microspheres were characterized for responses including drug release, particle size, and entrapment efficiency and floating time. Based on the results of the responses, the optimized composition was arrived using the response surface method graphical and numerical optimization method using design of experiments (DoE) software. Then, the optimized formulation (OFES) was prepared and evaluated for the four responses compared with predicted values to find the validity of the selected model. The optimized formulation was further analyzed for drug-excipient compatibility by fourier-transform infrared (FTIR), differential scanning calorimetry (DSC), and also analyzed by X-ray diffraction (XRD), scanning electron microscope (SEM) analysis. Further zeta potential and micrometric properties were also observed. The results for the formulation FES 1 to 9 found were, that particles size ranged from 0.192 to 0.277 μm, entrapment efficiency ranged from 68.65 ± 1.9 to 76.25 ± 3.2%, percentage drug release range was from 89.25 ± 0.24 to 93.68 ± 0 .25%, and floating time range was from 12 to 23 hours. As per the design, OFES an optimized formulation fitted with the concentration of Eudragit S 100 of 139.1 mg and stirring time of 1-hour. Regarding the kinetic release, the responses were best fitted with Higuchi model of R² value of 0.9795 with kinetic mechanism of non-fickian diffusion with R² value of 0.9499, indicating good linearity. The combination of different variables and their effects on responses were investigated well using factorial design, and an optimized formulation was developed for favipiravir.

Formulation, Characterization and In Vitro Evaluation of Mesalamine and Bifidobacterium bifidum Loaded Hydrogel Beads in Capsule System for Colon Targeted Delivery.

Mesalamine is a first-line drug for the treatment of inflammatory bowel diseases. However, its premature release associated with marketed formulations leads to adverse effects like gastric trouble, vomiting, and diarrhoea. To minimize these side effects, colon-targeted drug delivery is essential. Besides conventional pharmacotherapy, bifidogenic probiotics with anti-inflammatory activity has been reported to elicit a significant impact on the remission of ulcerative colitis. Bifidogenic probiotics being acid-labile necessitate developing a gastro-resistant formulation for enhancing the delivery of viable cells to the colon. The present study was aimed at developing a fixed-dose unit dosage form of mucoadhesive hydrogel beads loaded with mesalamine and Bifidobacterium bifidum further encapsulated in Eudragit® capsules for the targeted drug delivery at colonic pH. The hydrogel beads were prepared by ionotropic gelation, with the effect of single and dual-crosslinking approaches on various formulation characteristics studied. Standard size 00 Eudragit® gastro-resistant capsules were prepared and the dried beads were filled inside the capsule shells. The formulation was then evaluated for various parameters, including physicochemical characterization, in vitro biocompatibility and anti-inflammatory activity. No interaction was observed between the drug and the polymers, as confirmed through FTIR, XRD, and DSC analysis. The mean particle size of the beads was ~ 457-485µm. The optimized formulation showed a drug entrapment efficiency of 95.4 ± 2.58%. The Eudragit® capsule shells disintegrated in approximately 13min at pH 7.4. The mucoadhesive hydrogel beads sustained the drug release above 18h, with 50% of the drug released by the end of 12h. The optimized formulation demonstrated significant (p < 0.05) gastro-resistance, biocompatibility, sustained drug release, cell viability, and anti-inflammatory activity.

Development of Betulin-Loaded Nanostructured Lipid Carriers for the Management of Imiquimod-Induced Psoriasis.

Psoriasis is a complex and persistent autoimmune skin disease. The present research focused on the therapeutic evaluation of betulin-loaded nanostructured lipid carriers (BE-NLCs) towards managing psoriasis. The BE-NLCs were synthesized using the emulsification cum solidification method, exhibiting a spherical shape with a particle size of 183.5±1.82nm and a narrow size distribution window (PDI: 0.142±0.05). A high zeta potential -38.64±0.05mV signifies the relative stability of the nano-dispersion system. BE-NLCs show a drug loading and entrapment efficiency of 47.35±3.25% and 87.8±7.86%, respectively. In vitro release study, BE NLCs show a cumulative percentage release of 90.667±5.507% over BE-sol (57.334±5.03%) and BD-oint (42±4.58%) for 720min. In an ex vivo 24-h permeation study, % cumulative amount permeated per cm2 was found to be 55.667±3.33% from BE-NLCs and 32.012±3.26% from BE-sol, demonstrating a better permeability of 21.66% when compared to the standard formulation BD-oint. The in vivo anti-psoriatic activity in the IMQ-induced model shows topical application of BE-sol, BE-NLCs, and BD-oint resulted in recovery rates of 56%, 82%, and 65%, respectively, based on PASI (Psoriasis Area and Severity Index) score. Notably, BE-NLCs demonstrated a more significant reduction in spleen mass, indicating attenuation of the local innate immune system in psoriatic mice. Reductions in TNF-α, IL-6, and IL-17 levels were observed in both BE-sol and BE-NLCs groups compared to the disease control (DC) group, with BE-NLCs exhibiting superior outcomes (74.05%, 44.76%, and 49.26% reduction, respectively). Soy lecithin and squalene-based NLCs could be better carrier system for the improvement of the therapeutic potential of BE towards management of psoriasis.

Unlocking new dimensions in long-acting injectables using lipid mesophase-based beads

In this study, we explored the use of lipid mesophases (LMPs) as a biocompatible and biodegradable material for sustained drug delivery. Our hypothesis centered on leveraging the high surface-to-volume ratio of LMP-based beads to enhance strength, stability, and surface interaction compared to the LMP bulk gel. To modulate drug release, we introduced antioxidant vitamin E into the beads, influencing mesophase topologies and controlling drug diffusion coefficients. Four drugs with distinct chemical properties and intended for three different pathologies and administration routes were successfully loaded into the beads with a drug entrapment efficiency exceeding 80 %. Notably, our findings revealed sustained drug release, irrespective of the drugs' chemical properties, culminating in the development of an injectable formulation. This formulation allows direct administration into the target site, minimizing systemic exposure, and thereby mitigating adverse effects. Our approach demonstrates the potential of LMP-based beads for tailored drug delivery systems with broad applications in diverse therapeutic scenarios.

Formulation and Evaluation of Floating Microspheres

Gastro-retentive dosage forms have potential for use as controlled- release drug delivery systems. Gastro retentive floating drug delivery systems have a bulk density lower than that of gastric fluids and thus increase residence time of drug in stomach and provide controlled delivery of many drugs. The aim of the present study is formulation and characterization of floating microspheres using model drug. Floating microspheres were prepared by oil-in-water emulsion solvent evaporation technique using ethyl cellulose as release retarding polymers. The floating microspheres were evaluated for percentage yield (%), particle size, drug content, drug entrapment efficiency, in-vitro floating ability and in-vitro drug release studies. The surface morphology of prepared microspheres was characterized by scanning electron microscopy. The microspheres were found to be spherical in shape and porous in nature. Compatibility studies were performed by fourier transform infrared (FTIR) technique. The prepared microspheres showed prolonged drug release of 12 h and remain buoyant for more than 12 h. In-vitro release kinetics were studied in different release kinetics models like zero order, first order model. It was concluded that developed floating microspheres offers a suitable and practical approach for prolonged release of drug over an extended period of time and thus oral bioavailability, efficacy and patient compliance is improved

FORMULATION, CHARACTERIZATION AND OPTIMIZATION OF FOLIC ACID-TAILORED DAIDZEIN SOLID LIPID NANOPARTICLES FOR THE IMPROVED CYTOTOXICITY AGAINST COLON CANCER CELLS

Objective: The study aims to formulate and optimize daidzein-conjugated folic acid solid lipid nanoparticles (DZN-FA SLNs) to improve bioavailability and target site specificity for the treatment of colon cancer, a significant global health concern associated with high morbidity and mortality. Methods: DZN-FA SLNs were prepared using the microemulsion method. They were prepared and optimized using design expert software. Physicochemical characterization like differential light scattering (DLS), Fourier transformed infrared spectroscopy (FTIR), scanning electron microscope (SEM), In vitro drug release and In vitro cell line studies and accelerated stability studies were carried out in the optimized batch formulation. Results: The results indicated that particle size for optimized DZN-FA SLNs was in the range of 212 to 620 nm, zeta potential of-20 mV, drug entrapment efficiency of 72%. In vitro drug release for the prepared formulation showed 53% over 48 h. Conclusion: The optimized DZN-FA SLNs could aid in a better formulation targeting colon cancer cells, thereby reducing systemic effects. The optimized DZN-FA SLNs have demonstrated excellent inhibitory properties on Caco-2 cells, with an IC50 value of 10 µg/ml, offering a promising innovation in cancer treatment by providing targeted and effective therapy for colon cancer while minimizing the impact on normal cells.

Quality by Design Enabled Formulation Optimization of Rabeprazole Sodium Mucoadhesive Microcapsules for the Treatment of Gastroesophageal Reflux Disease

Aims: The present research describes the implementation of quality by-design principles for developing the mucoadhesive microcapsules of rabeprazole sodium for treating gastroesophageal reflux disease conditions. Background: In addition, a holistic QbD-based product development strategy was implemented, where the target product profile was defined based on desired product quality of mucoadhesive microcapsules. Based on TPP, the critical quality attributes were identified. The identification of CMAs was carried out with the help of risk assessment and factor screening exercises, which indicated drugpolymer ratio (X1), temperature (X2), and stirring speed (X3) as the influential factors. Methods: The mucoadhesive microcapsules of rabeprazole sodium were prepared by a solvent evaporation method, and 33 Box-Behnken optimization design was used for the optimization of the selected factors, and mucoadhesive microcapsules formulations were evaluated for particle size (μm), drug entrapment efficiency (%), mucoadhesion (%), and in vitro drug release (Q18h) in percentage characteristics. Mathematical data analysis was performed to fit the two-factor interaction model, and optimized mucoadhesive microcapsules formulation was selected. Results: The optimized mucoadhesive microcapsules indicated desired formulation characteristics with smaller particle size, good entrapment efficiency, better mucoadhesion, and sustained drug release characteristics. Conclusion: In a nutshell, the studies vouch for the successful development of mucoadhesive microcapsules for oral delivery of rabeprazole sodium which could be used to manage gastroesophageal reflux disease condition.

Optimization and characterization of xanthan gum based multiparticulate formulation for colon targeting

To optimize and characterize xanthan gum multi-particulate formulation for colon targeting, which increases the residence time at the absorbing surface of the colon. Xanthan gum was dispersed in cold water containing drug and was permitted to expand for 2 ​h. Sodium alginate was blended well in 10 ​ml of water. Xanthan gum solution containing the drug was added to sodium alginate solution and 0.3 ​ml of glutaraldehyde was added to the dispersion, with constant stirring. Then, polymer-drug solution was added dropwise into 5% w/v calcium chloride solution with continuous stirring, producing microspheres filtered by Whatman filter paper and dried at 30 ​°C–40 ​°C. Microspheres were performed by chemical cross-linking with glutaraldehyde, which increased the maximum drug entrapment efficiency up to 73.63 ​± ​0.65% with an increasing concentration of xanthan gum polymer 0.7% w/v for the optimized F6 batch. Better results were found by increasing the polymer concentration along with the glutaraldehyde concentration. The kinetics of drug release for the F6 batch was considered as an optimized batch because the regression value was found to be 0.997 in the peppas model. The accelerated stability study on the optimized F6 batch performed to learn whether the drug has any change during its period of usability. The polysaccharide remains intact in the stomach and intestine and the drug was released in the colon with low toxicity and biodegradability. The present studies showed that optimizing and characterizing xanthan gum multi-particulate formulation for colon targeting gives metronidazole the most effective and controlled delivery.

Sustained release of acyclovir from alginate-gellan gum and alginate-xanthan gum microbeads

In the current research, acyclovir-loaded microbeads were formulated via ionotropic gelation using sodium alginate-gellan gum and sodium alginate-xanthan gum. In the preparation of these acyclovir-loaded microbeads, aluminium chloride and barium chloride were used as cross-linking agents. All these ionotropically-gelled acyclovir-loaded alginate-gellan gum microbeads and alginate-xanthan gum microbeads exhibited good percent yields (85.07 ± 1.58 to 92.17 ± 3.02%) and drug entrapment efficiencies (74.09 ± 1.38 to 95.16 ± 3.37%). Acyclovir-loaded alginate-gellan gum microbeads exhibited comparatively smaller average particle sizes (0.54 ± 0.02 to 0.71 ± 0.03 mm) than those of acyclovir-loaded alginate-xanthan gum microbeads (0.60 ± 0.02 to 0.82 ± 0.04 mm). Acyclovir-loaded alginate-xanthan gum microbeads exhibited comparatively higher swelling than that of acyclovir-loaded alginate-gellan gum microbeads. A sustained pattern of acyclovir release over 240 min was noticed by these microbeads. Surface morphology analysis of the best microbeads formulation (on the basis of sustained acyclovir release data) was done by scanning electron microscopy (SEM). These kinds of ionotropically-gelled alginate-based microbeads might be advantageous to facilitate enhanced patient compliances with minimal dosing frequency and enhanced oral bioavailability.

Losartan potassium-loaded linseed polysaccharide-alginate-calcium silicate biomucoadhesive-floating beads for gastroretentive delivery

ABSTRACT The current research presents the formulation of losartan potassium-loaded biomucoadhesive-floating beads using sodium alginate (matrix-former), linseed polysaccharide (biomucoadhesive polymer) and calcium silicate (floatation-improving material). These losartan potassium-loaded beads showed 63.86 ± 0.93 to 95.33 ± 2.14% drug entrapment efficiency, 1.44 ± 0.04 to 1.72 ± 0.08 mm bead-size and 0.65 ± 0.06 to 0.81 ± 0.06 g/cm3 density. The biomucoadhesive-floating beads were characterized by SEM, FTIR and p-XRD. In gastric pH, losartan potassium-loaded beads presented excellent buoyancy, in vitro drug releasing over 10 h and good biomucoadhesivity. These biomucoadhesive-floating beads could be profitable to prolong gastroretention with sustained drug releasing.

Screening of important factors using factorial design to predict simvastatin loaded solid lipid nanoparticles

This study aims to optimize Simvastatin-loaded Solid Lipid Nanoparticles (SLNs) using a 2^k factorial design approach. Simvastatin, a widely used cholesterol-lowering drug, faces bioavailability challenges, prompting the use of nanotechnology for drug delivery. The study focuses on lipid concentration, surfactant concentration, and homogenization speed as critical factors influencing SLN characteristics. These factors were chosen based on their potential impact on SLN physicochemical properties like particle size, polydispersity index, and drug entrapment efficiency. Through systematic variation of factor levels, a matrix of experiments will be created, measuring responses (particle size, polydispersity index, and drug entrapment efficiency) for each run. Statistical analysis, including ANOVA, will assess factor significance and interactions. The study aims to reveal critical parameters affecting Simvastatin-loaded SLN formulation. The optimized formulation targets uniform and stable nanoparticles with enhanced drug entrapment, enhancing Simvastatin bioavailability. The factorial design method offers a systematic, resource-efficient approach for simultaneously screening and optimizing multiple factors, streamlining the experimental process.Top of Form

Critical Aggregation Concentration Can be a Predictor of Doxorubicin Delivery Performance of Self-Assembling Amphiphilic Peptides with Different Hydrophobic Tails

Amphiphilic peptides hold great potential as drug delivery systems. A popular peptide design approach has been to place amino acids in the peptide sequence based on their known properties. On the other hand, the directed discovery approach aims to screen a sequence space for a desired property. However, screening amphiphilic peptides for desirable drug delivery properties is not possible without a quantity that is predictive of these properties. We studied the predictive power of critical aggregation concentration (CAC) values on the drug delivery performance of a series of amphiphilic peptides with different hydrophobic tails and close CAC values. The CAC values were predicted by our previously developed model and doxorubicin was used as a model hydrophobic drug. All peptides showed close drug loading, entrapment efficiency, and release profile. They also formed similar spherical particles by assembling in reverse β-sheet arrangements regardless of drug presence. Moreover, the assembled particles were able to accumulate doxorubicin inside ordinary as well as drug-resistant breast cancer cells and enhance its toxicity up to 39 and 17 folds, respectively. It can be concluded that similar drug delivery properties displayed by the peptides can be attributed to their similar hydrophilic-lipophilic balance as reflected in their close CAC values.

P‐toluenesulfonychloride‐based niosomes for Amphotericin‐B against Leishmaniasis

AbstractNonionic‐surfactants have been reported as nanocarriers for delivering low bioavailable drugs at the target sites. In the current study, two new nonionic surfactants were synthesized to enhance the oral bioavailability of the low water‐soluble antifungal drug Amphotericin‐B. The hemolysis effect of nonionic surfactants on red blood cells and cytotoxicity against the 3T3 cell line was studied. Both surfactants have shown low hemolysis and cytotoxicity as compared to standard Tween 80. The morphology of drug‐loaded niosomes of nonionic surfactants 1 and 2 was studied by using atomic force microscopy (AFM), and both surfactants based vesicles were spherical, while their average sizes were measured by dynamic light scattering (DLS). The average size, zeta potential and polydispersity index (PDI) values of surfactants 1 and 2 were 282 ± 3 nm, −8 ± 1 mV, 0.26 and 287 ± 3 nm, −10 ± 1 mV, 0.24. The drug entrapment efficiency and critical micelle concentrations of nonionic surfactants were determined by using UV–visible spectroscopy. The structures of surfactants 1 and 2 were assessed through single‐crystal x‐ray crystallographic analysis, while Hirshfeld analysis was performed to study the intermolecular interactions of molecules, as well as the packing behavior of their crystals. The nonionic‐surfactant 1 was further tested for antileishmanial activity against Leishmania tropica promastigotes, in both drug‐loaded and unloaded niosomal vesicular forms. The nonionic surfactant 1 was found to be a potentanti‐leishmanial agent in the drug‐loaded form with IC50 = 3.02 ± 0.91 μM in comparison to their standard drugs Amphotericin‐B (IC50 = 3.8 ± 0.04 μM) and miltefosine (IC50 = 42.2 ± 0.6 μM) (p &lt; 0.1). These results, therefore, form the basis of further results towards efficient drug delivery against tropical disease Leishmaniasis.

Statistically developed stable Camptothecin-loaded Soluplus/TPGS mixed micelles for improved ovarian cancer treatment

In this research, Camptothecin-loaded mixed micelles (CPT-MMs) were formulated by combining Soluplus®, a novel amphiphilic excipient, with D-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS). The use of appropriate excipients is crucial in stabilizing micellar structures and improving drug entrapment efficiency. TPGS, with its ability to self-assemble into micelles, was an ideal candidate, and incorporating Soluplus further enhanced micelle stability and drug-loading capacity. A 32 full factorial design was employed to investigate the influence of key factors on particle size and %entrapment efficiency (%EE). The statistical analysis using Design Expert® VR software provided meaningful conclusions on the significance of each factor and their interactions, facilitating the successful optimization of CPT-MMs dispersion with improved drug delivery capabilities. The mean particle size, zeta potential, %drug loading capacity (%DLC), and (%EE) of CPT-MMs were 77.8 ± 2.67 nm, −23.4 ± 0.36 mV, 45.6 ± 1.78%, and 68.61 ± 1.8% respectively. CPT-MMs demonstrated sustained-release characteristics, preventing premature drug release and enhancing drug accumulation in tumor tissues, potentially optimizing CPT delivery for cancer treatment. Importantly, CPT-MMs dispersion exhibited lower hemolysis compared to plain CPT, indicating excellent biocompatibility and safety for intravenous administration. The sustained release of CPT from CPT-MMs dispersion may lead to reduced cytotoxicity and improved therapeutic efficacy. Additionally, the lyophilized formulation showed superior stability compared to the liquid micelles. In conclusion, the development of CPT-MMs presents a promising strategy for enhancing drug delivery and optimizing therapeutic outcomes in cancer treatment. The sustained-release feature, along with enhanced biocompatibility and stability, holds great potential for the clinical translation of these MMs as efficient drug delivery systems for ovarian cancer treatment.

Impact of umbelliprenin-containing niosome nanoparticles on VEGF-A and CTGF genes expression in retinal pigment epithelium cells.

To investigate the impact of niosome nanoparticles carrying umbelliprenin (UMB), an anti-angiogenic and anti-inflammatory plant compound, on the expression of vascular endothelial growth factor (VEGF-A) and connective tissue growth factor (CTGF) genes in a human retinal pigment epithelium (RPE)-like retina-derived cell line. UMB-containing niosomes were created, optimized, and characterized. RPE-like cells were treated with free UMB and UMB-containing niosomes. The IC50 values of the treatments were determined using an MTT assay. Gene expression of VEGF-A and CTGF was evaluated using real-time polymerase chain reaction after RNA extraction and cDNA synthesis. Niosomes' characteristics, including drug entrapment efficiency, size, dispersion index, and zeta potential were assessed. Free UMB had an IC50 of 96.2 µg/mL, while UMB-containing niosomes had an IC50 of 25 µg/mL. Treatment with UMB-containing niosomes and free UMB resulted in a significant reduction in VEGF-A expression compared to control cells (P=0.001). Additionally, UMB-containing niosomes demonstrated a significant reduction in CTGF expression compared to control cells (P=0.05). However, there was no significant reduction in the expression of both genes in cells treated with free UMB. Both free UMB and niosome-encapsulated UMB inhibits VEGF-A and CTGF genes expression. However, the latter demonstrates significantly greater efficacy, potentially due to the lower UMB dosage and gradual delivery. These findings have implications for anti-angiogenesis therapeutic approaches targeting age-related macular degeneration.

Development of an Antihypertensive Loaded Solid Lipid Nanoparticle

Solid lipid nanoparticles were prepared by using the solvent evaporation method. The prepared solid lipid nanoparticles of felodipine from different batches were weighed accurately and filled into appropriate-sized capsules for further evaluation. The prepared nanoformulation was tested in vitro for drug entrapment efficiency found to be 97-99% for the formulation with soya lecithin and glyceryl mono-stearate and percentage yield. The results of the in vitro drug release study for all formulations performed at gastric pH 1.2 indicated that the drug was released in an immediate manner within 60 minutes, which could be due to a burst effect or a faster rate of drug release due to smaller particle size SLN13 the concentration of Glycerol Monosterate- 576.522mg and Poloxamer 188. In vitro release data from standardised nanoformulations was fitted to various release kinetics models for the drug release mechanism. The optimised formulation demonstrated improved drug release and entrapment efficiency, and in vitro release data were fitted to various kinetic models to better understand the drug release mechanism. In vitro assay results were ranged between 76.5 to 96%, Zeta potential -40.75 ± 2.33 (mV) ± SD, entrapment efficiency 99.32. Accelerated stability studies for standardised nanoformulations were performed for 6 months in accordance with standard ICH guidelines, and no appreciable changes in the physical appearance, drug content, and in vitro drug release rates of the nanoformulations were observed. As a result of the study's evidence, it is concluded that felodipineloaded solid lipid nanoparticles are the best choice for hypertension.

Development of silibinin-loaded nanostructured lipid carriers for Alzheimer's disease induced by amyloid beta in Wistar rats.

Objective. The purpose of this study is to develop, optimize, and evaluate the in vivo effectiveness of orally administered silibinin-loaded nanostructured lipid carriers (SB-NLCs) in amyloid β-induced Alzheimer's disease in Wistar rats. Methods. The emulsification-solvent evaporation method was used for preparing the NLCs, using stearic acid, triacetin, and Cremophor® RH40. The statistical optimization of SB-NLCs was done using the Box-Behnken design (BBD). Then, the following parameters were evaluated: zeta potential, average size, in vitro drug release, and drug entrapment efficiency. Physicochemical properties of the optimized SB-NLCs were determined by FTIR, DSC, and P-XRD. The behavioral (OFT, NOR, MWM), histological (H&E, Congo Red), and biochemical (TAC, MDA, GSH) tests were conducted on 48 male Wistar rats. Results. The findings showed that the mean particle size, zeta potential and entrapment efficiency of optimized SB-NLCs were 194.71 ± 14.06 nm, -12.46 ± 0.25 mV, and 72.13% ± 1.41, respectively. XRD and DSC studies confirmed a reduction in the crystallinity of SB which occurred due to its embedment in the nanostructured lipid. The FTIR results indicated the lack of existence of any chemical interaction between the carrier components and the drug. Drug release in the external environment was slow and steady. Drug-containing nanoparticles showed good stability during three months of storage at 4 °C. The behavioral test of OFT showed no significant change between groups. The group treated with SB-NLCs showed a markedly higher discrimination rate compared to the Aβ group (p < 0.001). The time of the SB-NLC treated group in the target area was considerably more than the time of the SB and Aβ groups, respectively (p < 0.01, p < 0.001), in the MWM test. Histological and biochemical analysis revealed better results in the SB-NLC group as against the SB group. Conclusion. SB-NLCs can be considered as a promising formulation for the proper treatment of Alzheimer's disease in the oral drug delivery system.

Using a systematic and quantitative approach to generate new insights into drug loading of PLGA nanoparticles using nanoprecipitation.

The synthesis of drug-loaded PLGA nanoparticles through nanoprecipitation in solvent/antisolvent mixtures is well reported but lacks clarity in explaining drug loading mechanisms and the prediction of efficiency of drug entrapment. Various methods using physical parameters such as log P and solid-state drug-polymer solubility aim to predict the intensity of drug-polymer interactions but lack precision. In particular, the zero-enthalpy method for drug/polymer solubility may be intrinsically inaccurate, as we demonstrate. Conventional measurement of loading capacity (LC), expressed in weight ratios, can be misleading for comparing different drugs and we stress the importance of using molar units. This research aims to provide new insights and critically evaluate the established methodologies for drug loading of PLGA nanoparticles. The study employs four model drugs with varying solubilities in solvent/antisolvent mixtures, log P values, and solid-state solubility in PLGA: ketoprofen (KPN), indomethacin (IND), sorafenib (SFN), and clofazimine (CFZ). This study highlights that drug loading efficiency is primarily influenced by the drug's solubilities within the solvent system. We emphasise that both kinetic and thermodynamic factors play a role in the behaviour of the system by considering the changes in drug solubility during mixing. The study introduces a pseudo-constant K* to characterise drug-polymer interactions, with CFZ and SFN showing the highest K* values. Interestingly, while IND and KPN have lower K* values, they achieve higher loading capacities due to their greater solubilities, indicating the key role of solubility in determining LC.

FORMULATION AND EVALUATION OF CIPROFLOXACIN MICROSPHERES DESIGNED BY USING NATURAL POLYMERS BY IONIC GELATION TECHNIQUE

Objective: A definitive objective for supporting drug discharge is to expand the remedial movement of the medication while limiting its incidental effects. Microspheres have become a unique medicine delivery mechanism for several disorders in this area. The popular fluoroquinolone antibiotic, Ciprofloxacin, is used to treat a variety of bacterial illnesses. This research aims to create Ciprofloxacin microspheres with sustained drug delivery using natural gum polymers. Methods: To choose and assess the ideal formulation, a variety of formulations (F1–F8) were developed. This work was completed using an innovative technology, the Ionic Gelation method. Central Composite Design (CCD) used the quadratic forward regression approach to carry out the optimization. The evaluation tests include Particle size, Scanning Electron Microscopy (SEM), FTIR, Percentage yield, Drug content, Drug Entrapment effectiveness and in vitro dissolution studies. Results: It was discovered that the best formulation was F4. From optimization, the ANOVA was found to be significant. The uneven, spherical structure of microspheres with a rough outer surface is confirmed by SEM investigation. The absence of drug-polymer interaction is confirmed by the FTIR. The formulation F4 was deemed ideal due to its high drug entrapment efficiency, drug content and maximal drug release (89.25% in 12 h). Conclusion: Due to the least plasma half-life, this drug is designed as microspheres thus maximizing the therapeutic activity and minimizing the negative effects. In this regard, microspheres have emerged as novel drug-delivery systems for various diseases. It maintains effective dose concentration, eliminates night-time dosage and decreases side effects, thus optimizing drug therapy.

Design and Application of pH-Responsive Liposomes for Site-Specific Delivery of Cytotoxin from Cobra Venom.

Current immunotherapies with unexpected severe side effects and treatment resistance have not resulted in the desired outcomes for patients with melanoma, and there is a need to discover more effective medications. Cytotoxin (CTX) from Cobra Venom has been established to have favorable cytolytic activity and antitumor efficacy and is regarded as a promising novel anticancer agent. However, amphiphilic CTX with excellent anionic phosphatidylserine lipid-binding ability may also damage normal cells. We developed pH-responsive liposomes with a high CTX load (CTX@PSL) for targeted acidic-stimuli release of drugs in the tumor microenvironment. The morphology, size, zeta potential, drug-release kinetics, and preservation stability were characterized. Cell uptake, apoptosis-promoting effects, and cytotoxicity were assessed using MTT assay and flow cytometry. Finally, the tissue distribution and antitumor effects of CTX@PSL were systematically assessed using an in vivo imaging system. CTX@PSL exhibited high drug entrapment efficiency, drug loading, stability, and a rapid release profile under acidic conditions. These nanoparticles, irregularly spherical in shape and small in size, can effectively accumulate at tumor sites (six times higher than free CTX) and are rapidly internalized into cancer cells (2.5-fold higher cell uptake efficiency). CTX@PSL displayed significantly stronger cytotoxicity (IC50 0.25 μg/mL) and increased apoptosis in than the other formulations (apoptosis rate 71.78±1.70%). CTX@PSL showed considerably better tumor inhibition efficacy than free CTX or conventional liposomes (tumor inhibition rate 79.78±5.93%). Our results suggest that CTX@PSL improves tumor-site accumulation and intracellular uptake for sustained and targeted CTX release. By combining the advantages of CTX and stimuli-responsive nanotechnology, the novel CTX@PSL nanoformulation is a promising therapeutic candidate for cancer treatment.