Diffusion Release Research Articles

Smart Mucoadhesive Film Former from Seeds of Arachis Hypogea and Its In-Built Properties for Pharmaceutical Applications

Aim: Isolation of novel biopolymer from Arachis hypogea seeds to be used as bio-excipient in formulation of nanosized Topiramate loaded bio-flexy films for epilepsy treatment. Method: Formulations containing nanosized Topiramate: Arachis hypogea biopolymer (in ratios of 1:0.5, 1:1; 1:3, 1:5, 1:6, 1:10) (FAO1-FAO6) were prepared by solvent casting method. Results: Arachis Hypogea Biopolymer showed percentage yield of 20% ±0.01. The biopolymer was brown in color, odourless, partially soluble in water. Its colour changing point was found to be 210ºC±2. It was tested positive for proteins and carbohydrates, amino acids were not present. Evaluation parameters of nanosized Topiramate loaded bio-flexy films containing Arachis hypogea biopolymer (FAO1-FAO6) revealed Thickness: 0.022 mm±0.004 to 0.044±0.003 mm, Folding Endurance: 140-169, Surface pH: 7.01±0.03 to 7.01±0.02, Weight Uniformity: 0.006±0.04 to 0.036±0.02, Drug Content Uniformity: 85.4%±0.68 to 93.4%±0.50, Swelling Percentage: 73%±0.6 to 89%±0.4, Percentage Moisture Uptake (PTU): 1.8%±0.10 to 2.4%±0.08, Mucoadhesion time: 45-150 minutes, Mucoretention time: 75-210 minutes. The drug release pattern for formulations FAO1-FAO6 containing Arachis hypogea biopolymer based on the T50% and T80% was found to be FAO2 (1:1) > FAO5 (1:6) > FAO6 (1:10) > FAO1 (1:0.5)> FAO4 (1:5) > FAO3 (1:3). Conclusion: Based on all above-mentioned evaluation parameters, FAO2 (containing Topiramate: Arachis hypogea biopolymer (1:1)) Bio-flexy film having R2 =0.9215, Higuchi Matrix as best fit model, follows Fickian Diffusion (Higuchi Matrix) release mechanism, T50%: 44.52 hrs., T80%: 46.14 hrs. using BITS Software. Stability study revealed stable formulations. Isolated Arachis hypogea biopolymer showed in-built filmability, mucoadhesivity properties, was non-reactive and suitable for Soft Palatal Drug Delivery.

Effect of polyethylene glycol and nano clay on swelling, diffusion, network parameters and drug release behavior of interpenetrating network copolymer

AbstractControlled release of a drug from a biocompatible nontoxic polymer at a predetermined rate by maintaining a constant drug level for a specific time period causes its maximum utility with reduced side effect and more efficient cure of the disease. Accordingly, several composite hydrogels were synthesized by free radical crosslink copolymerization of acrylic acid (AA), acrylamide (AM), and N'N‐methylene bis acrylamide (MBA, crosslinker) in water in the presence of varied amounts of polyethylene glycol (PEG) and nano sized sodium montmorillonite (NaMMT) clay. The structures of the hydrogels were characterized. The effect of the synthesis and process parameters on the swelling, diffusion, network parameters, and drug release properties of the polymer networks were studied. The hydrogel containing 3.2 wt% NaMMT clay and 24 wt% PEG showed the best equilibrium swelling ratio (33.2 g/g), drug entrapment efficiency (86%), and drug release properties (96.6% in 30 h at pH of 7.4) for a model drug riboflavin. The results indicate a significant improvement of swelling and drug release properties of the polymer in the presence of PEG and NaMMT clay in the gel network.

Phase transited asymmetric membrane floating nanoparticles: a means for better management of poorly water-soluble drugs.

Effective remedy to gastrointestinal (GI) side effects caused by poorly water-soluble drugs remains a challenge. Researching for novel techniques to reduce these side effects and increase patient adherence to medical treatment is of interest. The current study aims to develop an innovative nano-sized gastro-retentive drug delivery for better management of poorly water-soluble drugs. A non-disintegrating ibuprofen-asymmetric membrane floating nanoparticle (Ibuprofen-AMFNP) was prepared by phase inversion technique to increase the gastric residence of the drug. Powder characterization, solubility, in vitro buoyancy, effect on in vivo inflammatory markers, and polymer diffusibility studies were conducted on the prepared formulation. All UV-spectrophotometric analysis was accomplished through a fiber optic system. The prepared Ibuprofen-AMFNPs were in the nano range of 114.45nm ±1.31nm. The formulation was buoyant for 12h in the dissolution media indicating increased gastric residence, had better solubility and powder characteristics compared to the pure drug. Scanning electron microscopy revealed an outer non-porous and inner porous asymmetric membrane. Ibuprofen-AMFNP followed Higuchi drug release kinetics (p=0.9925) and had a Fickian diffusion release mechanism (n=0.05). Polymer diffusibility study showed that the 24h stored formulation had faster drug release with no lag time (-923.08nm/h) compared to a fresh formulation (2526.32nm/h). The prepared nano-formulation showed a higher percentage of anti-inflammatory (85.144%) effect compared to the pure drug (78.336%). Ibuprofen-AMFNP is envisioned to help reduce drug-related GI side effects, improve drug delivery, and thereby increase patient adherence to medical treatment.

Mathematical modelling of drug release from a porous granule

Understanding drug release from pharmaceutical granules is vital to the development of targeted release profiles. A model describing diffusion and solubility-limited drug dissolution and release from a porous spherical granule of drug and excipient is considered. Radially varying porosity and initial concentration profiles which can arise in pharmaceutical granules are incorporated. A range of boundary-value and moving-boundary-value problems arise, depending on the relationship between the drug saturation concentration in the solvent medium and the initial drug concentration and porosity profiles. The model is derived in detail for the case where the initial drug concentration is greater than the drug saturation concentration in all parts of the granule. In this case, a moving boundary forms at the granule surface and propagates inwards, separating an unextracted inner core from a shell region which undergoes extraction via diffusion. The full model is non-dimensionalised and analysed using asymptotic methods and numerical solution. A leading-order model is derived by exploiting a small parameter corresponding to the ratio of the drug saturation concentration to the maximum initial concentration in the granule, allowing estimation of the time taken for the moving boundary to reach the granule centre. The behaviour of the full model is considered by solving it using a boundary immobilisation method and the finite element method for a range of parameters and comparing to the leading-order model. Finally, the model outputs for the moving boundary position and normalised drug release are compared with experimental data from the literature.

Applying design of experiments (DoE) on the properties of buccal film for nicotine delivery

Abstract Design of experiments is used to optimize ratios between deproteinized natural rubber latex, Eudragit® NM 30 D, and pectin for nicotine buccal film with dependent variables as moisture content, moisture uptake, and swelling index in simulated saliva 3 and 5 h. Mathematical models were linear for moisture content and moisture uptake, while swelling index in simulated saliva 3 and 5 h was a quadratic model. Optimized polymer ratio was 0.319:0.362:0.319, respectively. Experimental values were 13.17 ± 0.92%, 3.96 ± 0.84%, 112.58 ± 22.63%, and 124.69 ± 8.01% for dependent variables, respectively. The buccal film showed high swelling at pH 7 and swelling–deswelling behaviors in a water/ethanol environment. The surface pH, weight, and thickness were 8.11, 63.28 ± 6.18 mg, and 219.87 ± 44.28 µm, respectively. Nicotine content was found as 10.22 ± 0.46 mg/4 cm2. Maximum cumulative nicotine release was 9.82 ± 0.94 mg/4 cm2. Kinetic model fitted to the Korsmeyer-Peppas model and release exponent was 0.36, representing that release mechanism was controlled by Fickian diffusion release.

Optimization and characterization of hepatoprotective andrographolide microspheres in the necrotic rat model

This study aimed to develop controlled release drug delivery of oral andrographolide encapsulated in microspheres, targeted against degenerative hepatic disorder. Ionotropic gelation technique was used to prepare andrographolide loaded Chitosan/Na-Alginate microspheres. The final drug formulation was optimized based on the statistical modeling used in the study. SEM, DSC, and XRD studies revealed a spherical formulation with a smooth surface morphology and increased thermal stability. Mean particle size, drug entrapment efficiency, and cumulative drug release from the optimized formulation were observed to be 37.46 ± 2.3 μm, 88.13 ± 3.6%, and 93.04 ± 5.1%, respectively, and manifesting steady-state release profile up to 12 h with zero-order kinetics and Non-Fickian diffusional release. In-vivo studies show a remarkable effect in elevated liver enzyme levels, and hepatocellular necrosis in CCl4 intoxicated Wistar Rats. Findings from this study suggest that andrographolide microspheres could be a potential delivery system with high oral bioavailability and sustained drug release profile against hepatic necrosis.

Theoretical study of diffusional release of a dispersed solute from a hollow cylindrical polymeric matrix

An exact solution for the release kinetic of a solute from inside a hollow cylindrical polymeric matrix into an infinite medium has been developed, when the initial concentration of the solute (A) is greater than the solubility limit (Cs). A combination of analytical and numerical methods was used to calculate the solute concentration profile and the release rate. The model was developed for two different strategies: 1) the release medium is flowing through the hollow cylinder in which boundary layer may be neglected, 2) the release medium inside the hollow cylinder is stagnant and the boundary layer should be considered. The results indicated that the release profiles were close to the constant release rate after a typical burst release. Also, the release profile from a solid cylindrical matrix and a hollow cylinder was compared. The results indicated that the hollow cylindrical matrix is a promising carrier when zero-order release is desirable. The present model demonstrates the potential of the hollow cylindrical matrix as a suitable geometry for sustained drug delivery systems.

Hollow CoP/FeP4 Heterostructural Nanorods Interwoven by CNT as a Highly Efficient Electrocatalyst for Oxygen Evolution Reactions.

Electrolysis of water to produce hydrogen is crucial for developing sustainable clean energy and protecting the environment. However, because of the multi-electron transfer in the oxygen evolution reaction (OER) process, the kinetics of the reaction is seriously hindered. To address this issue, we designed and synthesized hollow CoP/FeP4 heterostructural nanorods interwoven by carbon nanotubes (CoP/FeP4@CNT) via a hydrothermal reaction and a phosphorization process. The CoP/FeP4@CNT hybrid catalyst delivers prominent OER electrochemical performances: it displays a substantially smaller Tafel slope of 48.0 mV dec−1 and a lower overpotential of 301 mV at 10 mA cm−2, compared with an RuO2 commercial catalyst; it also shows good stability over 20 h. The outstanding OER property is mainly attributed to the synergistic coupling between its unique CNT-interwoven hollow nanorod structure and the CoP/FeP4 heterojunction, which can not only guarantee high conductivity and rich active sites, but also greatly facilitate the electron transfer, ion diffusion, and O2 gas release and significantly enhance its electrocatalytic activity. This work offers a facile method to develop transition metal-based phosphide heterostructure electrocatalysts with a unique hierarchical nanostructure for high performance water oxidation.

Formulation, Design and Optimization of Glycerosomes for Topical Delivery of Minoxidil

Background: Present work reports the formulation design and optimization of minoxidil loaded glycerosomes for topical application. The delivery system enhances the vesicular properties of vesicles by modifying the fluidity of lipid bilayer. The major component of formulation consists of phospholipid, glycerol, and cholesterol. Methodology: Glycerosomes were prepared by using lipid film hydration method. Prepared formulations were optimized using Box behnken 32 full factorial experimental designs. Two independent variables were selected which were Sonication time (X1), and Glycerol Concentration (X2) and with respect to these two dependent variables were selected which were % cumulative drug release after eight hours (Y1), and Entrapment efficiency (Y2). Nine formulations of (G1-G9) were prepared based on factorial design for optimization. Result and Discussion: Prepared formulations were evaluated in terms of surface analysis, charge distribution, encapsulation efficiency, in-vitro diffusion studies, stability testing and release kinetics. The fabricated glycerosomes found to possess entrapment efficiency in the range of 70.29±0.75 to 87.91±0.23%, cumulative drug release: 73.12 to 89.39%; a shelf life of 356 days at 4± 1°C and show higuchi release kinetics, fickian diffusion. Conclusion: As glycerol present in formulation in high quantity, this is itself used as humectant, emollient and penetration enhancer. So this formulation is best suitable for topical delivery of drugs.

Synthesis and Characterization of a Fe3O4@PNIPAM-Chitosan Nanocomposite and Its Potential Application in Vincristine Delivery.

In this research, we conducted a systematic evaluation of the synthesis parameters of a multi-responsive core-shell nanocomposite (Fe3O4 nanoparticles coated by poly(N-isopropylacrylamide) (PNIPAM) in the presence of chitosan (CS) (Fe3O4@PNIPAM-CS). Scanning electron microscopy (SEM) was used to follow the size and morphology of the nanocomposite. The functionalization and the coating of Fe3O4 nanoparticles (Nps) were evaluated by the ζ-potential evolution and Fourier Transform infrared spectroscopy (FTIR). The nanocomposite exhibited a collapsed structure when the temperature was driven above the lower critical solution temperature (LCST), determined by dynamic light scattering (DLS). The LCST was successfully shifted from 33 to 39 °C, which opens the possibility of using it in physiological systems. A magnetometry test was performed to confirm the superparamagnetic behavior at room temperature. The obtained systems allow the possibility to control specific properties, such as particle size and morphology. Finally, we performed vincristine sulfate loading and release tests. Mathematical analysis reveals a two-stage structural-relaxation release model beyond the LCST. In contrast, a temperature of 25 °C promotes the diffusional release model. As a result, a more in-depth comprehension of the release kinetics was achieved. The synthesis and study of a magnetic core-shell nanoplatform offer a smart material as an alternative targeted release therapy due to its thermomagnetic properties.

Hierarchical Core‐Shell N‐Doped Carbon@FeP4‐CoP Arrays as Robust Bifunctional Electrocatalysts for Overall Water Splitting at High Current Density

AbstractExploring non‐precious metal‐based electrocatalysts at high current density and stability is an urgent issue for sustainable H2 production. Here, hierarchical core‐shell N‐doped carbon encapsulated array‐like FeP4 and CoP active components have been fabricated in situ on the surface of nickel foam (NC@FeP4‐CoP/NF) by etching sheet‐like ZIF‐67 arrays, Prussian analog formation, and phosphating in turns. The crystallinity, hierarchical heterostructure, and chemical state have been carefully discussed. Electrochemical studies demonstrate that the catalyst displays excellent electrocatalytic activity and durability in electrochemical oxygen evolution reaction (η20 = 218 mV) and hydrogen evolution reaction (η10 = 116 mV), better than most previously reported bifunctional catalysts. Moreover, the bifunctional catalyst only needs 1.72 and 1.80 V cell voltages at 500 and 1000 mA cm−2 respectively, together with a good catalytic stability at 500 mA cm−2 for 48 h, implying potential commercialization prospects. This excellent electrocatalytic performance is mainly attributed to the distinctive hierarchical structure as well as core‐shell NC encapsulated FeP4‐CoP active sites, which can enhance the charge transport rate, inhibit the exfoliation of the active materials, provide a larger active surface area, and facilitate electrolyte diffusion and gas release.

Synthesis of chitosan/Al-MCM-41 nanocomposite from natural microcline as a carrier for levofloxacin drug of controlled loading and release properties; Equilibrium, release kinetic, and cytotoxicity

The presented study focused on the production of a promising delivery system for levofloxacin drug (LVX) of significant loading capacity, controlled release rate, and low preparation cost. Synthesis of Al-MCM-41 from natural microcline as innovative mesoporous structure and integrated it in nanocomposite with chitosan (CS/Al-MCM) resulted in a hybrid structure of enhanced technical properties as drug carrier of significant biocompatibility. Natural microcline was used in the synthesis of Al-MCM-41 by hydrothermal treatment in the existence of an organic template for 24 h at 110 °C. The product was integrated with chitosan into a composite (CS/Al-MCM) which was applied as a carrier for LVX with a loading capacity of 480.6 mg/g which is higher than chitosan (188.8 mg/g) and Al-MCM-41 (340 mg/g). The loading reactions of CS/Al-MCM followed the Pseudo-Second-order kinetic behavior and Langmuir isotherm properties. The theoretical models suggested a homogenous and monolayer loading process that involved chemical and physical reactions of exothermic and spontaneous properties. The CS/Al-MCM showed a significant release profile for 180 h with a maximum release percentage of 96.2%. The LVX release properties followed the Korsmeyer-Peppas behavior with a diffusion exponent related to both diffusion and erosion release mechanisms. The cytotoxicity properties of CS/Al-MCM and LVX loaded CS/Al-MCM declared their safety and biocompatible effect on human bronchial epithelia.

Mn-doped NiCo2S4 nanosheet array as an efficient and durable electrocatalyst for oxygen evolution reaction

The development of self-supported nanosheet materials with porous multiple active sites has enormous potential for the application of oxygen evolution reaction (OER). Herein, we reported a three-dimensional (3D) porous nanosphere Mn-NiCo2S4/NF catalyst for OER. As a result, the simple Mn doping strategy results in good electrocatalytic performance and outstanding stability. During the OER, the Mn-NiCo2S4/NF only needs a small overpotential of 220 mV (40 mV lower than pure NiCo2S4/NF) to achieve the current density of 10 mA cm−2, which is mainly due to a large number of exposed active sites and adequate pathways for mass diffusion and oxygen gas release. Moreover, Mn doping optimizes the electronic structure and thus facilitates electron transport, leading to superior electrocatalytic performance. The catalyst exhibits incredible corrosion resistance in 1 M KOH solution for 60 h or more. This work provides a valuable method to synthesize a low cost, high-efficiency, and corrosion resistant transition metal electrocatalyst for oxygen evolution using heteroatom doping strategy.

Study and modeling of hydrogen release from Ti, Zr, Ni, Pd, Pt during linear heating

New the experimental results of thermally stimulated hydrogen release (TCHR) from plane-parallel plates of Ti, Zr, Ni, Pd, Pt metals with various thicknesses (0.05–1 mm), pre-saturated with hydrogen, under linear heating (1 °C s−1) presented. The electrolytic and Sieverts method for saturate were used. Theoretical models for diffusion and desorption hydrogen release from flat metal samples into vacuum with linear heating were developed. In this case, the processes of diffusion and thermal desorption were taken into account to select the optimal conditions and experimental methods. The TSHR spectra simulated using the MATLAB software package to test the consistency of theory with experiment. By modeling in MATLAB using both the developed models and experimental TSHR spectra, the activation energies of desorption, diffusion and decomposition of hydrides, as well as the preexponential factors in the diffusion and kinetic equations, were determined.

Application of Central Composite Design for Development and Optimization of Eflornithine Hydrochloride-loaded Sustained Release Solid Lipid Microparticles

Topical application of eflornithine hydrochloride (EFH) is the only available non-hormonal and non-systemic choice available for hirsutism treatment. EFH has low permeability (log P is -2.9). The current investigation's objective is the development of solid lipid microparticles-based sustained topical release delivery with enhanced permeability of eflornithine hydrochloride. EFH-loaded solid lipid microparticles (EFH-SLM) composed of Monecol PC and Softemul 165 using emulsion solvent evaporation technique. The central composite design has been applied to explore an optimized EFH-SLM, which was incorporated into cream (EFH-SLM-C) and evaluated for in-vitro drug release and permeation analysis. Design expert software illustrated that an optimized EFH-SLM having desirability function (0.806) could be achieved using 1:3.74 drug: lipid (w/w) (X1), 1.84% surfactant concentration (X2), and 3.5 h stirring time (X3), which would illustrate entrapment efficiency (74.97%), drug loading (15.84%), mean diameter (102.8 µm) and process yield (78.07%). EFH-SLM-C revealed biphasic fickian diffusion release of 16.95% within 0.5 h, 52.31% in the next 4 h followed by sustained release of 88.75% over 24 h. This was confirmed by release exponent 0.411 (n < 0.45) for Korsmeyer-Peppas. In-vitro steady-state flux (Jss) (µgcm-2h-1) from EFH-C and EFH-SLM-C were 17.27 and 36.65 while apparent permeability coefficient (Papp) (cmh-1) was 0.046 and 0.0977, respectively. EFH-SLM-C could be a promising strategy for augmented permeation and sustained release with minimization of dose, frequency of application, and local adverse effects.

Release Mechanisms and Kinetic Models of Gypsum-Sulfur-Zeolite-Coated Urea Sealed with Microcrystalline Wax for Regulated Dissolution.

In this study, a mineral-based coated urea was fabricated in a rotary pan coater using a mixture of gypsum/sulfur/zeolite (G25S25Z50) as an effective and low-cost coating material. The effects of different coating compositions on the dissolution rate of urea and the crushing strength and morphology of the coated urea were investigated. A 25:25:50 (wt %) mixture of gypsum/sulfur/zeolite (G25S25Z50) increased the coating effectiveness to 34.1% with the highest crushing strength (31.06 N). The effectiveness of coated urea was further improved to 46.6% with the addition of a microcrystalline wax (3%) as a sealant. Furthermore, the release mechanisms of various urea fertilizers were determined by fitting the release profiles with six mathematical models, namely, the zeroth-order, first-order, second-order, Higuchi, Ritger & Peppas, and Kopcha models. The results showed that the release mechanism of the uncoated urea and all other coated urea followed the Ritger & Peppas model, suggesting the diffusional release from nonswellable delivery systems. In addition, due to the increased mass-transfer resistance, the kinetic constant was decreased from 0.2233 for uncoated urea to 0.1338 for G25S25Z50-coated urea and was further decreased to 0.0985 when 3% Witcovar 146 sealant was applied.

Fabrication and characterization of cuminaldehyde-loaded electrospun gliadin fiber mats

This work's objective was to develop a novel type of gliadin electrospun fiber with antibacterial properties by incorporating cuminaldehyde in the fibrous structure. Gliadin fibers containing various concentrations of cuminaldehyde were fabricated via an electrospinning process. The morphology and size of the fibers were affected by the concentration of incorporated cuminaldehyde. An optimum value was selected as the highest concentration of cuminaldehyde (20%, w/w). 1H NMR spectroscopy indicated the presence of incorporated cuminaldehyde in gliadin fibers. In addition, the FTIR spectroscopy suggested the occurrence of hydrogen interactions between CO bonds of cuminaldehyde and N–H bonds of gliadin at 1651 and 3293 cm−1. Confocal Raman spectroscopy and X-ray diffraction revealed a homogenous distribution of cuminaldehyde in the amorphous cuminaldehyde-loaded gliadin fibers with almost no crystalline peaks of cuminaldehyde. Moreover, the gliadin fibers enhanced the thermostability of cuminaldehyde. The hydrophobic cuminaldehyde-loaded gliadin fiber showed a non-Fickian diffusion release, antibacterial activity against Staphylococcus aureus (PTTC 1112) Escherichia coli (PTCC 1399), and is non-toxic to the ASCs. These results confirm the capacity of cuminaldehyde-loaded gliadin fibers for being used in food applications.

IBUPROFEN LOADED ORGANOGEL: DEVELOPMENT AND CHARACTERIZATION

Objective: This study aimed to develop and in vitro characterize an organogel (OG) loaded Ibuprofen.
 Methods: Organogel (OG) composed of water, isooctane, sorbitan esters, sorbitan monopalmitate (Span-40), and poly(oxyethylene) sorbitan monostearate (Polysorbate-60) was loaded with Ibuprofen. The partial phase behavior of ibuprofen OG was studied to optimize the formulation composition. 1.0% w/w Ibuprofen loaded OG were characterize for rheological, in vitro release and stability study.
 Results: Phase diagram showed an isotropic gel region at low water contents, which converted to emulsion on increasing water quantity. The rheological properties of the OG incorporating 1.0% w/w Ibuprofen shows the presence of two Tg’s and elastic behavior of gel, reflects the presence of an entangled network of aqueous tubules. The fractal dimension df value of 2.1 and 2.3 was obtained for the two curves (elastic and storage modulus), which is indicative of the formation of the densest gel structure. The diffusional release exponent (n) was found to be ~0.7 (0.5<n<1), which is indicative of non-Fickian, anomalous diffusion of the drug from the OG. The in vitro drug release exhibited release @ 7.04%/h 0.7/cm2 from the OG. Ibuprofen containing OG was stable for 28 d in terms of chemical potency and gel stiffness at 4 °C and room temperature (~25 °C).
 Conclusion: The study indicates the potential of OG for improved transdermal delivery of Ibuprofen.

Self-assembled membrane-polymer nanoparticles of top-notch tissue tolerance for the treatment of gastroesophageal reflux disease

Controlled release technology has continuously attracted attention as a strategy to deliver active agents to specific internal body regions with attendant cost-effectiveness among other intriguing merits. Here, drug-loaded nanoparticles (NPs) are synthesized for ultimate application in the treatment of gastroesophageal reflux disease (GERD), leveraging the benefits of controlled release strategy. To achieve this, eggshell membranes (ESMs) were extracted and combined with chitosan (CHS) to rationally obtain self-assembled CHS–ESM NPs that served as a novel nanocarrier to effectively compartmentalize a GERD-therapeutic drug famotidine (FTD) and form self-assembled FTD@CHS–ESM NPs. Advantageously, the proof-of-concept FTD@CHS–ESM NPs offer superlative tissue tolerance. The cumulative FTD release is 89% after 12 h at pH 1.2, suggesting the capability of FTD@CHS–ESM NPs for effectual controlled drug release; a testimonial of the effective compartmentalization of FTD in the nanocarrier. Furthermore, the release of FTD from the FTD@CHS–ESM NPs is best described by Higuchi square root model, in a non-Fickian diffusional release mechanism (n = 0.584 and 0.582 in pH 1.2 and pH 6.8, respectively). The drug release system demonstrated in this work, therefore, holds strong promise for the oral nanomedical treatment of GERD in vivo, and promotes the rational synthesis of organic-based biocompatible nanomaterials for biomedical application.

Optimization of Hydroxy Propyl Methyl Cellulose and Carbomer In Diltiazem Hydrochloride Mucoadhesive Buccal Film

Diltiazem hydrochloride (HCl) is a category of calcium channel blocker used as an antihypertensive agent. Diltiazem HCl is a low bioavailable drug due to high first-pass metabolism and a short half-life (3-5 hours); hence mucoadhesive buccal film was made to overcome this weakness. Bioavailability of Diltiazem HCl increase if the buccal preparations can contact the mucosa for a sufficient time. Therefore, in this study, two polymers are combined to obtain good film characteristics, especially residence time and mucoadhesive strength. This study was aimed to optimize Hydroxy Propyl Methyl Cellulose (HPMC) and Carbomer's amount in Diltiazem HCl mucoadhesive buccal film. The formulas were prepared by the solvent casting method and optimized with design expert software. The release kinetics and mechanism were evaluated using DDSolver program. The optimum amount of polymer obtained from optimization was 40 mg of HPMC and 10 mg of Carbomer. The optimum formula's swelling index was 4.18. The mucoadhesive strength was 53.07 gF, and the mucoadhesive residence time was 529.33 min. The FTIR spectra showed there was no interaction between Diltiazem HCl and other excipients. Thus it did not disturb the therapeutic effect. Based on the DDSolver statistical parameters and curve-fitting, the dissolution model of Diltiazem HCl from buccal mucoadhesive film follows Korsmeyer-Peppas. The release exponent (n) is 0.55, which shows a non-fickian/anomalous diffusion release mechanism. These mechanisms represent drug release controlled by a combination of diffusion and erosion.