Solvent Evaporation Technique Research Articles

Formulation and evaluation of transdermal patch of carbamazepine

Transdermal drug delivery system (TDDS) is a widely accepted mode of drug delivery method due to various advantages and one of the novel routes for systemic delivery of drugs through intact skin. Topical drug administration is a systemic and localized method of delivering drugs through skin and is considered an attractive alternative to oral and parenteral routes. The aim of present study was to formulate and evaluate Matrix type transdermal drug delivery system (TDDS) of Carbamazepine was prepared by the solvent evaporation technique. Several batches were prepared by using combination of HPMC E-15, Eudragit RL-100, and Ethyl Cellulose different ratios. Propylene glycol was used as plasticizer and DMSO was incorporated as a permeation enhancer. These Formulated transdermal patches were characterized for their physicochemical parameters like thickness, weight variation, folding endurance, percentage moisture uptake, Percentage moisture uptake and In vitro drug release studies were examined. Among the above all formulation F6 was chosen as a best Formulation, because this optimised formulation showed satisfactory drug content, physical characteristic for its thickness, weight uniformity, percentage moisture content, percentage moisture uptake, and maximum % of drug release i.e., 93.95 % in 12 hours. The optimized formulation (F6) showed maximum highest percentage of drug release.

Research on Formulation and Evaluation of Floating Microspheres

The purpose of this study is to design and evaluate a floating multipart oral delivery system for diltiazem hydrochloride that can provide sustained release. The aim of the work is also to study various parameters that influence the behaviour of floating multiparticles in an oral dosage form. Floating microspheres were prepared by a non-aqueous emulsifying solvent evaporation technique using ethyl cellulose and Eudragit RS-100 asthe rate-controlling polymer. In vitro activity was evaluated using standard pharmacopoeia and other tests such as drug-polymer compatibility, (%)yield, particle size analysis, drug entrapment efficiency, surface topography, in vitro buoyancy and release studies. The results show that the mixing ratio of the components in the organic phase affected the size, size distribution (199-320 µm), drug concentration(59-84%), percent yield (57-77%) and drug. Liberation microsphere (45-99aftern12 hours) and swimming time > 12 hours. The best results were obtained in the ratio drug: polymer Eudragit RS-100 (1:3). Good in vitro floating behaviour was observed in most cases, and various drug release patterns could be achieved by varying the polymer ratio, which was optimized to match the target release profile. Stability studies showed no significant change in the drug content of the formulation even after 3months. The data obtained in this study therefore suggest a floating dose of micro particles

Solid Lipid Nanoparticles: A Review of their Biomedical Applications and Preparation.

Solid lipid nanoparticles (SLNs) are gaining significant attention in the pharmaceutical industry due to their biocompatibility and biodegradability, making them a popular functional nanocarrier. SLNs are a popular nanocarrier due to their ability to bypass the spleen and liver, offer high drug stability, and improve bioavailability, sterilization, immobilization, targeted drug release, and biocompatible ingredients. This article discusses various SLN preparation techniques, including high shear homogenization, hot homogenization, cold homogenization, microemulsion-based, solvent evaporation, solvent emulsification-evaporation, supercritical fluid-based, spray drying, double emulsion, and precipitation techniques, focusing on methodological aspects. This review discusses the physicochemical behavior of SLNs, including drug loading, release, particle size, stability, cytotoxicity, and cellular uptake, and their major biomedical applications.

Systematic Scrutinization of Vital factors for the Development of Efficient Cisplatin-Quercetin Loaded Bionanomicelles

The present work aims to optimize and assess the Cisplatin (CIS) and Quercetin (QCT)-loaded biodegradable polymeric nanomicelles (PNM). The development of a quantitative method for the estimation of CIS and QCT in pharmaceutical dosage form was another objective. The aluminum plates coated with silica gel F254 used for separation of both the drugs employing Toluene: Methanol: Ethyl acetate: DMF: Triethylamine (5:0.5:3.5:1:1 drop % v/v/v/v/v) as mobile phase. Results of the validation parameter indicate that the developed method was precise, accurate, and robust. CIS and QCT-loaded PNM formulated using solvent evaporation technique employing poly lactic-co-glycolic acid (PLGA) 50:50. The Quality by Design (QbD) was accomplished to identify the critical manufacturing attributes and critical process parameters. Optimization of the formulation was performed by central composite design using particle size and % encapsulation efficiency as dependent variables. The amount of PLGA and Span selected as independent variables. Statistically substantial variables identified using regression analysis and analysis of variance. A diffusion study revealed that optimized nanomicelles were capable to sustain the drug release up to 8h. Zeta sizer, TEM confirmed the stability and nano-sized nanoparticles. CIS-QCT PNM was found to be an alternate route to systemic treatment.

Formulation and Evaluation of Betulin Loaded Transdermal Patches

Objectives: To develop and evaluate Transdermal patches of Betulin along with various polymers for controlled release action. Method: Suitable method such as Solvent Casting Technique of Film Casting Technique are used for preparation of Transdermal patch. Result: The prepared Transdermal patches were transparent, smooth, uniform and flexible. The method adopted for preparation of system was found satisfactory. Conclusion: Various formulations were developed by using hydrophilic and hydrophobic polymers like HPMC E5 and EC respectively in single and combinations by solvent evaporation technique with incorporation of penetration enhancer such as dimethylsulfoxide and dibutyl phthalate as plasticizer. Formulation F7 containing equal ratio of HPMC E5: EC (5:5) showed maximum percentage drug content 95.44%. A suitable UV Spectroscopy method for the analysis of Betulin was developed. Betulin showed maximum absorption at wave length 215 nm in isotonic phosphate buffer (pH 7.4) solutions. The pre-formulation studies involving description, solubility, melting point, partition coefficient of the drug were found to be comparable with the standard. The Transdermal patch of Betulin was prepared successfully by solvent evaporation method. Transdermal patch of Betulin for Transdermal drug delivery was evaluated. Calibration curve was obtained; Transdermal film was prepared, overcome limitations regarding bioavailability of drug was done. Keywords: Controlled DDS, Transdermal DDS, Betulin, Transdermal Patch, solvent evaporation method.

Formulation, Optimization and Evaluation of Solid Dispersion of Deferasirox Using Factorial Design

Deferasirox, an oral iron-chelating agent, is a poorly soluble drug (Biopharmaceutical Classification System class II) having insufficient solubility in physiological fluids resulting in low bioavailability of the drug. The idea behind the present study was to explore the prospects of solid dispersion as a prolific method to enhance the dissolution rate of drug using a water soluble polymer. The solid dispersion was prepared by the solvent evaporation technique using Polyvinyl pyrrolidone with different drug to carrier and solvent ratio. Formulations were characterized through attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR), differential scanning calorimetry (DSC), Powder X-ray diffraction (XRD), and in vitro release studies. A 32 factorial design was implemented to obtain optimum solubility, % yield, and optimization of solid dispersion (SD) also quantitates the influence of PVP on the solubility and dissolution profile. Thedrug-to-carrier and solvent ratio was chosen as independent variable, while %yield, drug content, and saturation solubility were chosen as dependent variables. The results showed that the optimized formulation of SD-DFX was able to significantly enhance its solubility. The SD containing a dispersion of Deferasirox with PVP show an exceptional rise in the solubility. This study describes the development of solid dispersion that significantly improved the solubility and bioavailability of DFX. The FTIR studies indicate the interaction between the drug and polymer. The DSC and XRD analysis indicated that the drug was in an amorphous state when dispersed in the polymer. It is resolved that the SD method significantly improves the solubility and dissolution rate, which could also be exploit for other poorly water soluble drug candidates. Keywords: Deferasirox , Polyvinyl pyrrolidone, solid dispersion, Factorial design, Solubility

Preparation and Preliminary Analysis of Several Nanoformulations Based on Plant Extracts and Biodegradable Polymers as a Possible Application for Chronic Venous Disease Therapy.

Nanotechnology is one of the newest directions for plant-based therapies. Chronic venous disease often predisposes to long-term and invasive treatment. This research focused on the inclusion of vegetal extracts from Sophorae flos (SE), Calendulae flos (CE), and Ginkgo bilobae folium (GE) in formulations with PHB and PLGA polymers and their physicochemical characterization as a preliminary stage for possible use in the development of a complex therapeutic product. The samples were prepared by an oil-water emulsification and solvent evaporation technique, resulting in suspensions with high spreadability and a pH of 5.5. ATR-FTIR analysis revealed bands for stretching vibrations (O-H, C=O, and C-H in symmetric and asymmetric methyl and methylene) in the same regions as the base components, but switched to high or low wavenumbers and absorbance, highlighting the formation of adducts/complexes between the extracts and polymers. The obtained formulations were in the amorphous phase, as confirmed by XRD analysis. AFM analysis emphasized the morphological peculiarities of the extract-polymer nanoformulations. It could be noticed that, in the case of SE-based formulations, the dominant characteristics for SE-PHB and SE-PLGA composition were the formation of random large (SE-PHB) and smaller uniform (SE-PLGA) particles; further on, these particles tended to aggregate in the case of SE-PHB-PLGA. For the CE- and GE-based formulations, the dominant surface morphology was their porosity, generally with small pores, but larger cavities were observed in some cases (CE- and GE-PHB). The highest roughness values at the (8 µm × 8 μm) scale were found for the following samples and succession: CE-PHB < SE-PLGA < SE-PHB-PLGA. In addition, by thermogravimetric analysis, impregnation in the matrix of compression stockings was evaluated, which varied in the following order: CE-polymer > SE-polymer > GE-polymer. In conclusion, nine vegetal extract-polymer nanoformulations were prepared and preliminarily characterized (by advanced physicochemical methods) as a starting point for further optimization, stability studies, and possible use in complex pharmaceutical products.

Electromagnetic drop-on-demand (DoD) technology as an innovative platform for amorphous solid dispersion production

Production of amorphous solid dispersions (ASDs) is an effective strategy to promote the solubility and bioavailability of poorly water soluble medicinal substances. In general, ASD is manufactured using a variety of classic and modern techniques, most of which rely on either melting or solvent evaporation. This proof-of-concept study is the first ever to introduce electromagnetic drop-on-demand (DoD) technique as an alternative solvent evaporation-based method for producing ASDs. Herein 3D printing of ASDs for three drug-polymer combinations (efavirenz-Eudragit L100-55, lumefantrine-hydroxypropyl methylcellulose acetate succinate, and favipiravir-polyacrylic acid) was investigated to ascertain the reliability of this technique. Polarized light microscopy, differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD), and Fourier Transform Infrared (FTIR) spectroscopy results supported the formation of ASDs for the three drugs by means of DoD 3D printing, which significantly increases the equilibrium solubility of efavirenz from 0.03 ± 0.04 µg/ml to 21.18 ± 4.20 µg/ml, and the equilibrium solubility of lumefantrine from 1.26 ± 1.60 µg/ml to 20.21 ± 6.91 µg/ml. Overall, the reported findings show how this new electromagnetic DoD technology can have a potential to become a cutting-edge 3D printing solvent-evaporation technique for on-demand and continuous manufacturing of ASDs for a variety of drugs.

Development and Evaluation of a Novel Hyaluronic Acid and Chitosan-modified Phytosome for Co-delivery of Oxymatrine and Glycyrrhizin for Combination Therapy.

Multidrug resistance (MDR) of cancer cells is a major obstacle to efficient cancer chemotherapy. Combination therapy is expected to enhance the anticancer effect and reverse MDR. Numerous patents involve different kinds of nanoparticles for the co-delivery of multiple chemotherapeutics, but the FDA has approved none. In this study, oxymatrine (OMT) and glycyrrhizin (GL) were co-loaded into phytosomes as the core of nanocarriers, and the shell was cross-linked with chitosan (CS) and hyaluronic acid (HA) with the capability for the controlled, sequential release and the targeted drug uptake. Phospholipid complexes of OMT and GL (OGPs) were prepared by a solvent evaporation technique and could self-assemble in an aqueous solution to form phytosomes. CS and HA were sequentially coated on the surface of OGPs via electrostatic interactions to obtain CS coated OGPs (CS-OGPs) and HA modified CS-OGPs (HA-CS-OGPs), respectively. The particle size and zeta potential were measured to optimize the formulations. In vitro cytotoxicity and cellular uptake experiments on HepG2 cells were performed to evaluate the anticancer activity. OGPs were obtained with nano-size around 100 nm, and CS and HA coating on phytosomes could change the particle size and surface potential. The drug loading of OMT and GL showed that the nanocarriers could maintain a fixed ratio of 1:1. The in vitro release experiments indicated the release of OMT and GL was pH-dependent and sequential: the release of OMT from CS-OGPs and HA-CS-OGPs was significantly increased at pH 5.0 compared to the release at pH 7.4, while GL exhibited sustained released from CS-OGPs and HA-CS-OGPs at pH 5.0. Furthermore, in vitro cytotoxicity and cellular uptake experiments on HepG2 cells demonstrated that the co-delivery system based on phytosomes had significant synergistic anti-tumor activities, and the effects were enhanced by CS and HA modification. The delivery of OMT and GL via HA-CS-OGPs might be a promising treatment to reverse MDR in cancer therapy.

Formulation, Evaluation and Study of Super Disintegrants effect on Olmesartan Medoxomil Fast Dissolving Tablets

The current research was to enhance solubility and dissolution rate of the slightly soluble drug, Olmesartan medoxomil, solid dispersions by physical mixing, solvent evaporation and kneading techniques, with soluplus. The solid dispersions prepared are tested for flow properties, drug content, and particle size. In vitro dissolution studies were carried out to analyse the drug release from solid dispersions. Crystal morphology, drug and polymer interaction for selected solid dispersions was studied by FT-IR and DSC analysis. Fast-dissolving tablets were formulated by using optimized solid dispersions using different concentrations of sodiumstarch glycolate, crosscarmellosesodium, and crospovidone as superdisintegrants using direct compression technique. The tablets prepared are tested for Weight variation, friability, disintegration, content uniformity and harness. The mechanism and kinetics of drug release from the fast-dissolving tablets were tested by in-vitro dissolution studies. The current research proves that combining solid dispersions along with the use of superdisintegrants is novel approach to formulate of Olmesartan medoxomil fast-dissolving tablets.

Design Optimization and Pharmacokinetic Study of Eletriptan Hydrobromide Loaded Solid Lipid Nanoparticle Nasal Gel Targeted to Brain

In the present research work, Eletriptan Hydrobromide(E-HBr)-loaded solid lipid nanoparticles (SLN’s) incorporated in a gel was prepared by emulsification solvent evaporation technique to enhance the uptake of E-HBr to brain via intra-nasal (i.n.) route and the formulations were evaluated for particle size, polydispersibility index, zeta potential, drug entrapment efficiency, in-vitro drug release, and stability of the optimized formulation. All the parameters evaluated were within the acceptable range. In-vitro drug release for the optimized gel formulation was found to be 92.45% after 12hr and was fitted to the Higuchi model with a very high correlation coefficient (R2=0.995). Pharmacokinetics studies were performed on albino male Wistar rats and the concentration of E-HBr in brain and blood plasma was measured by HPLC. The brain/blood ratio at 0.5h for E-HBr Opt.SLN’s i.n., E-HBr sol. i.n., and E-HBr sol. oral. were found to be 2.35, 1.19 and 0.80 respectively, indicating the drug transported directly from nose-to-brain, by bypassing the blood–brain barrier in the olfactory region present in the nasal cavity. The maximum concentration of drug in brain (Cmax) after i.n. administration of E-HBr-SLN gel was found to be (21465.87±1110.66ng/ml, Tmax 8.45hr) significantly higher than that achieved after oral administration (6797.23±842.86ng/ml, Tmax 7hr), and i.n. (16451.53±3792.40ng/ml, Tmax 7.69 hr) administration of E-HBr sol. The highest drug-targeting efficiency (2.35%) and direct transport percentage (66.05%) was found with E-HBr-SLN’s as compared to the other formulations. Higher DTE (%) and DTP (%) suggest, that E-HBr-SLN gel had better brain targeting efficiency as compared to other formulations.

Natural Polymer-Based Nanogel for pH-Responsive Delivery of Sorafenib Tosylate in Hemangiosarcoma.

Smart nanomedicinal treatment for cancer manifests a solubility challenge with inherent nanoscale size and nonspecific release with stimuli-responsive potential. This is the limelight in novel chemotherapy to pursue physiochemical differences between the tumor microenvironment (TME) and normal cells, which introduces active groups of nanocarriers responding to various stimuli, endowing them with concise responses to various tumor-related signals. The nanogels were successfully prepared by a modified solvent evaporation technique. Nine batches were formulated by changing the chitosan concentration (12, 14, 16mg/ml) and sonication time (5, 10, 15min). The formulations were optimized for particle size and zeta potential with high percent entrapment efficiency (%EE) through Central Composite Design software. The optimized batch F7 had a 182-nm size and high zeta potential (64.5mV) with 98% EE. The drug release of F7 was higher at pH 6 (97.556%) than at pH 7.4 (45.113%). The pharmacokinetic study shows that the release follows the Hixon plot model (R2 = 0.9334) that shifts to zero order (R2 = 0.9149). The nanogel F7 was observed for stability and showed an absence of color change, phase separation, and opacity for 6months. In the present study, the pH difference between cancer cells and normal cells is the key point of the smart nanogel. This study is promising but challenging depending on the in vivo study. The nanogel was successfully prepared and evaluated for pH-responsive release. As hemangiosarcoma commonly occurs in dogs, this formulation helps to limit the difficulties with administration.

Mucoadhesive chitosan-poly (lactic-co-glycolic acid) nanoparticles for intranasal delivery of quetiapine – Development & characterization in physiologically relevant 3D tissue models

Quetiapine hemifumarate (QF) delivery to the CNS via conventional formulations is challenging due to poor solubility and lower oral bioavailability (9 %). Similarly, many other second-generation antipsychotics, such as olanzapine, clozapine, and paliperidone, have also shown low oral bioavailability of <50 %. Hence, the present work was intended to formulate QF-loaded biodegradable PLGA-NPs with appropriate surface charge modification through poloxamer-chitosan and investigate its targeting potential on RPMI-2650 cell lines to overcome the limitations of conventional therapies. QF-loaded poloxamer-chitosan-PLGA in-situ gel (QF-PLGA-ISG) was designed using emulsification and solvent evaporation techniques. Developed QF-PLGA-ISG were subjected to evaluation for particle size, PDI, zeta potential, ex-vivo mucoadhesion, entrapment efficiency (%EE), and drug loading, which revealed 162.2 nm, 0.124, +20.5 mV, 52.4 g, 77.5 %, and 9.7 %, respectively. Additionally, QF-PLGA formulation showed >90 % release within 12 h compared to 80 % of QF-suspension, demonstrating that the surfactant with chitosan-poloxamer polymers could sustainably release medicine across the membrane. Ex-vivo hemolysis study proved that developed PLGA nanoparticles did not cause any hemolysis compared to negative control. Further, in-vitro cellular uptake and transepithelial permeation were assessed using the RPMI-2650 nasal epithelial cell line. QF-PLGA-ISG not only improved intracellular uptake but also demonstrated a 1.5–2-fold increase in QF transport across RPMI-2650 epithelial monolayer. Further studies in the EpiNasal™ 3D nasal tissue model confirmed the safety and efficacy of the developed QF-PLGA-ISG formulation with up to a 4-fold increase in transport compared to plain QF after 4 h. Additionally, histological reports demonstrated the safety of optimized formulation. Finally, favorable outcomes of IN QF-PLGA-ISG formulation could provide a novel platform for safe and effective delivery of QF in schizophrenic patients.

Self-micellizing solid dispersion of thymoquinone with enhanced biopharmaceutical and nephroprotective effects

The present study was designed to develop a self-micellizing solid dispersion (SMSD) containing Thymoquinone (TQM), a phytonutrient obtained from Nigella sativa seeds, aiming to improve its biopharmaceutical and nephroprotective functions. The apparent solubility of TQM in polymer solutions was used to choose an appropriate amphiphilic polymer that could be used to make an SMSD system. Based on the apparent solubility, Soluplus® was selected as an appropriate carrier, and mixing with TQM, SMSD-TQM with different loadings of TQM (5–15%) was made by solvent evaporation and freeze-drying techniques, respectively, and the formulations were optimized. The optimized SMSD-TQM was evaluated in terms of particle size distribution, morphology, release characteristics, pharmacokinetic behavior, and nephroprotective effects in a rat model of acute kidney injury. SMSD-TQM significantly improved the dissolution characteristics (97.8%) of TQM in water within 60 min. Oral administration of SMSD-TQM in rats exhibited a 4.9-fold higher systemic exposure than crystalline TQM. In a cisplatin-induced (6 mg/kg, i.p.) acute kidney-damaged rat model, oral SMSD-TQM (10 mg/kg) improved the nephroprotective effects of TQM based on the results of kidney biomarkers and histological abnormalities. These findings suggest that SMSD-TQM might be efficacious in enhancing the nephroprotective effect of TQM by overcoming biopharmaceutical limitations.

Formulation and Evaluation of &lt;i&gt;Amomum sublatum&lt;/i&gt; Leaf Oil Incorporated Pluronic Matrix Type Transdermal Patches in Percutaneous Absorption

A matrix type of transdermal patch formulations having different types of hydrophilic, hydrophobic polymer components Diclofenac potassium (Diclofenac K) served as the model drug and penetration enhancer for topical delivery in this research, employing the USP7 apparatus for dissolution studies. Transdermal patches loaded with Amomum sublatum leaf volatile oil (utilized penetration enhancer) were formulated using the solvent evaporation technique, incorporating varying amounts of pluronic F-127 and ethyl cellulose based on 15 formulations designed by the Box Behnken model. The prepared patches underwent evaluation for various physicochemical parameters, including tensile toughness, moisture content, and moisture uptake. In vitro diffusion studies were conducted using the USP7 apparatus dedicated to transdermal drug release investigations. The optimized formulation, F10, exhibited a drug release of 82% over 24 hours in the in vitro diffusion study. All the transdermal matrix-type formulations demonstrated satisfactory results, indicating that the developed matrix-type transdermal patch, containing different polymers and the A. sublatum leaf volatile oil penetration enhancer, holds potential for transdermal delivery in the treatment of pain and swelling.

Physio-chemical and biological Characterizations of 4 Bromo – 4'Chloro Benzylidene Aniline μ-crystals for Engineering Utilities

4 Bromo—4’Chloro Benzylidene Aniline - as per suggestion it is named as 4B4CBA; Schiff based organic material has been synthesized and successfully grown by slow solvent evaporation technique. The orthorhombic crystal system of the grown crystal with space group Pccn is confirmed and cell parameters of the grown crystal of 4B4CBA is found by single crystal X-ray diffraction (XRD) analysis. The forming of the C-Cl and C-Br stretching vibrations at 719 cm−1 and 538 cm−1 in Fourier Transform Infra-Red (FTIR) study reveal the confirmation of 4B4CBA compound. The CHNSO analysis shows the presence of element in the 4B4CBA. The lower cutoff wavelength and wide optical absorption window of 4B4CBA exhibit the suitability of the present material for the projective opto-electronic applications. Nonlinear optical efficiency for different micro-crystalline of 4B4CBA is determined by second harmonic generation (SHG) experiment and is also compared with Potassium Dihydrogen Phosphate - KDP material. The electrical studies confirm that the 4B4CBA crystal possess low dielectric constant values at high frequency region. The experiment of photo-conductivity confirms the nature of the photo-conductivity of 4B4CBA crystal. The Scanning electron microscopy (SEM) analysis reveals the morphology of 4B4CBA crystal.

Regulating Tumor-Associated Macrophage Polarization by Cyclodextrin-Modified PLGA Nanoparticles Loaded with R848 for Treating Colon Cancer.

This study aimed to develop a novel and feasible modification strategy to improve the solubility and antitumor activity of resiquimod (R848) by utilizing the supramolecular effect of 2-hydroxypropyl-beta-cyclodextrin (2-HP-β-CD). R848-loaded PLGA nanoparticles modified with 2-HP-β-CD (CD@R848@NPs) were synthesized using an enhanced emulsification solvent-evaporation technique. The nanoparticles were then characterized in vitro by several methods, such as scanning electron microscopy (SEM), differential scanning calorimetry (DSC), Fourier transform infrared (FTIR) spectroscopy, particle size analysis, and zeta potential analysis. Then, the nanoparticles were loaded with IR-780 dye and imaged using an in vivo imaging device to evaluate their biodistribution. Additionally, the antitumor efficacy and underlying mechanism of CD@R848@NPs in combination with an anti-TNFR2 antibody were investigated using an MC-38 colon adenocarcinoma model in vivo. The average size of the CD@R848@NPs was 376 ± 30 nm, and the surface charge was 21 ± 1 mV. Through this design, the targeting ability of 2-HP-β-CD can be leveraged and R848 is delivered to tumor-supporting M2-like macrophages in an efficient and specific manner. Moreover, we used an anti-TNFR2 antibody to reduce the proportion of Tregs. Compared with plain PLGA nanoparticles or R848, CD@R848@NPs increased penetration in tumor tissues, dramatically reprogrammed M1-like macrophages, removed tumors and prolonged patient survival. The new nanocapsule system is a promising strategy for targeting tumor, reprogramming tumor -associated macrophages, and enhancement immunotherapy.

Comprehensive Characterization and Comparative Assessment of Carvedilol Solid Dispersions: Insights into Enhanced Bioavailability and Stability Profiles

Carvedilol, a non-selective beta-adrenergic antagonist, poses a challenge in achieving optimal bioavailability due to its poor aqueous solubility. This study aimed to enhance the solubility and dissolution rate of carvedilol through the formulation and evaluation of solid dispersions. Various solid dispersion formulations were prepared using different carriers and methods, including solvent evaporation, fusion, and spray-drying techniques. The prepared formulations were systematically characterized using Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and scanning electron microscopy (SEM) to investigate drug-carrier interactions, solid-state changes, and morphological characteristics. Evaluation of the formulated solid dispersions involved in vitro dissolution studies, solubility enhancement assays, and stability assessments. Dissolution profiles revealed significantly improved drug release rates for the solid dispersion formulations compared to the pure drug. The solubility of carvedilol was notably enhanced in the solid dispersion systems, indicating improved drug dissolution behavior. Stability studies demonstrated the robustness of selected formulations against environmental factors over an extended period. Moreover, pharmacokinetic studies conducted in animal models showcased enhanced bioavailability of carvedilol from the optimized solid dispersion formulation compared to the conventional drug formulation. This comprehensive investigation provides valuable insights into the development of carvedilol solid dispersions, elucidating the influence of formulation variables on drug solubility, dissolution, stability, and ultimately, bioavailability enhancement. The findings underscore the potential of solid dispersion technology as a promising strategy to overcome the solubility challenges associated with carvedilol, paving the way for improved therapeutic efficacy and patient compliance.

MICROBALLOONS: A PROMISING APPROACH FOR GASTRORETENTIVE DRUG DELIVERY SYSTEM AND THEIR ADVANTAGES, LIMITATIONS, RECENT ADVANCEMENT IN DRUG DELIVERY SYSTEM, PATENTS AND FUTURE ASPECTS

The key objective of the present review was to collect the latest literature on technological advancements towards microballoons as novelistic buoyant drug delivery systems. Microballoons are hollow microspheres with a potential approach for gastric retention, offering controlled release of the drugs. It offers prominent targeting of drugs in the stomach. More significantly, it is an anticipated drug delivery system in the gastrointestinal tract’s upper section. At a high pH environment, this drug delivery system improves the solubility of less soluble drugs. It is an innovative and authenticated drug delivery system, specifically for those drugs which are unable to tolerate the acidic pH. The microballoons are developed by several techniques like Solvent Evaporation, Solvent Diffusion-Evaporation, Solvent Diffusion and Spray Drying techniques, to develop the space of empty inner core. Moreover, this manuscript covers significance, limitations, applications, list of polymers used, characterization, formulation design and evaluation parameters of microballoons.

Formulation and Evaluation of Microspheres Drug Delivery for Multiple Sclerosis Disease Condition

AMultiple sclerosis (MS) is chronic inflammatory disease that affecting the central nervous system (CNS) which leads to the degeneration of oligodendrocytes, neurons, and myelin over time. Being the foremost reason of neurological disability multiple sclerosis has affected about 2.5 million humans around the world. MS is mainly seen in early adulthood and adults in their middle age. Disease modifying agents are being used in treatment of relapsing multiple sclerosis. Medications that reduce the severity of the disease are frequently utilized as standard therapies. The immune system is the primary focus of modern MS treatments. However, researchers are putting more effort into designing novel CNS-focused treatments. Therefore, under the current scenario, an alternative route for drug delivery is required, one that provides a speedy onset of action and then maintains the drug release over an extended period. The desired prolong-acting intramuscular injecting stable fingolimod HCl microspheres to treat MS were formulated using solvent evaporation technique. Further, based on the number of factors to be optimized, formulation was prepared using solvent evaporation. Additionally, the formulated fingolimod microspheres were characterized for the size distribution of particle, particle surface morphology, and lyophilization of formulated microspheres. Post lyophilization, the formulated microspheres evaluation was done for efficiency of entrapment, drug release in-vitro, and stability parameters. Furthermore, in-vivo studies were performed on suitable animal models for the optimized formulation.