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Solid dispersions have achieved significant interest as an effective means of enhancing the dissolution rate and thus the bioavailability of a range of weakly water-soluble drugs. Solid dispersions of weakly water-soluble drugs with water-soluble carriers have lowered the frequency of these problems and improved dissolution. Solid dispersion is a s...
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... Solid dispersions employing hydrophilic carriers are commonly exploited to heighten the dissolution rate and bio-absorption of the drugs with low aqueous solubility [46]. Notably, the biopharmaceutical classification system (BCS) class II and class IV drugs have critical solubility issues and thus pose a challenge in drug delivery. ...
Inulin (IN) is a prebiotic oligosaccharide reported in diverse sources of nature. The major sources encompass chicory, Jerusalem artichoke, onions, barley, garlic, rye, and wheat. The literature also reported its promising biological activities, e.g., antidiabetic, anticancer, antioxidant, immune-regulator and prebiotic for improving intestinal function, regulation of blood lipids, and so on. IN's molecular flexibility, stabilization, and drug-targeting potential make it a unique polymer in pharmaceutical sciences and biomedical engineering. Further, its nutritional value and diagnostic application also widen its scope in food and medical sciences. The hydroxyl groups present in its structure offer chemical modifications, which could benefit advanced drug delivery such as controlled and sustained drug delivery, enhancement of bioavailability, cellular uptake, etc. This work reviews the isolation and purification of IN. The study also provides glimpses of the chemistry, chemical modification, and applications in pharmaceutical sciences and drug delivery.
... Drugs in the crystal form can be changed into an amorphous form using a solid dispersion. Solid dispersions of the drugs tend to have increased water-solubility since the particle size has decreased and porosity has increased [34]. Formulations with a low loading efficiency contain an extensive amount of polymer, which increases the size of the formulations and makes it challenging for the patient to swallow [35]. ...
Expandable films for stomach-specific delivery were developed to release quercetin, a flavonoid with in vivo gastroprotective effects, in a prolonged release fashion. We found that a solid dispersion containing quercetin and the hydrophilic polymers polyvinylpyrrolidone (PVP K30) at a 1:8 w/w ratio had approximately 1,400-fold enhanced solubility (27.84 mg/mL). The quercetin solid dispersions were loaded into expandable starch/chitosan films by solvent casting method, which combined chitosan with various types of starch (pre-gelatinized maize starch, glutinous rice starch, and rice starch). We found that using pre-gelatinized maize starch-based film led to the optimized formulation. During an 8-hour exposure to simulated stomach fluid, the formulation could unfold, swell, and release 80% of contained quercetin sustainably. Compared to indomethacin, the quercetin-loaded films exhibited a similar anti-inflammatory effect against RAW 264.7 macrophage cells in a dose-dependent manner. The obtained quercetin expandable films are promising as a stomach-specific delivery system.
... Solid dispersion also has disadvantages including poor physical and chemical stability, which can result in degradation. Once the polymers used in solid dispersions absorb moisture, structural changes can occur to result in decreased solubility and instability [158][159][160], hindering scale-up and subsequent manufacturing potential. SMEDDS form an oil-in-water microemulsion and consist of a homogenous mixture of oils and surfactants which [161] enhance the bioavailability of poorly soluble drugs by protecting against enzymatic degradation and improving their membrane permeability across the mucosal barrier of the intestine [161]. ...
Inflammatory diseases present a serious health challenge due to their widespread prevalence and the severe impact on patients' lives. In the quest to alleviate the burden of these diseases, nuclear factor erythroid 2-related factor 2 (Nrf2) has emerged as a pivotal player. As a transcription factor intimately involved in cellular defense against metabolic and oxidative stress, Nrf2's role in modulating the inflammatory responses of immune cells has garnered significant attention. Recent findings suggest that Nrf2's ability to alter the redox status of cells underlies its regulatory effects on immune responses. Our review delves into preclinical and clinical evidence that underscores the complex influence of Nrf2 activators on immune cell phenotypes, particularly in the inflammatory milieu. By offering a detailed analysis of Nrf2's role in different immune cell populations, we cast light on the potential of Nrf2 activators in shaping the immune response towards a more regulated state, mitigating the adverse effects of inflammation through modeling redox status of immune cells. Furthermore, we explore the innovative use of nanoencapsulation techniques that enhance the delivery and efficacy of Nrf2 activators, potentially advancing the treatment strategies for inflammatory ailments. We hope this review will stimulate the development and expansion of Nrf2-targeted treatments that could substantially improve outcomes for patients suffering from a broad range of inflammatory diseases.
... Hence, this technology is widely acknowledged as a precious means of enhancing the dissolution properties of poorly water-soluble drugs. Over the years, significant progress has been made in understanding solid dispersion, yet its commercial application remains limited [103]. Inulin has found its application in enhancing the bioavailability of various weakly water-soluble drugs, such as curcumin. ...
In recent years, inulin has gained much attention as a promising multifunctional natural biopolymer with numerous applications in drug delivery, prebiotics, and therapeutics. It reveals a multifaceted biopolymer with transformative implications by elucidating the intricate interplay between inulin and the host, microbiome, and therapeutic agents. Their flexible structure, exceptional targetability, biocompatibility, inherent ability to control release behavior, tunable degradation kinetics, and protective ability make them outstanding carriers in healthcare and biomedicine. USFDA has approved Inulin as a nutritional dietary supplement for infants. The possible applications of inulin in biomedicine research inspired by nature are presented. The therapeutic potential of inulin goes beyond its role in prebiotics and drug delivery. Recently, significant research efforts have been made towards inulin's anti-inflammatory, antioxidant, and immunomodulatory properties for their potential applications in treating various chronic diseases. Moreover, its ability to reduce inflammation and modulate immune responses opens new avenues for treating conditions such as autoimmune disorders and gastrointestinal ailments. This review will attempt to illustrate the inulin's numerous and interconnected roles, shedding light on its critical contributions to the advancement of healthcare and biomedicine and its recent advancement in therapeutics, and conclude by taking valuable insights into the prospects and opportunities of inulin.
... This parameter is in turn related to the surface area available for dissolution: in the case of a dissolution rate slower than the absorption rate, the dissolution step clearly becomes the rate-limiting step in the absorption process [5]. To improve the speed and completeness of the adsorption of problematic drugs, many strategies have been proposed, such as particle size reduction and the preparation of solid dispersions or salts, micelles, or liposomes [6][7][8]. However, inorganic-organic hybrids stand out compared to the other proposed systems ...
Poorly water-soluble drugs represent a challenge for the pharmaceutical industry because it is necessary to find properly tuned and efficient systems for their release. In this framework, organic–inorganic hybrid systems could represent a promising strategy. A largely diffused inorganic host is hydroxyapatite (HAP, Ca10(PO4)6(OH)2), which is easily synthesized with different external forms and can adsorb different kinds of molecules, thereby allowing rapid drug release. Hybrid nanocomposites of HAP nanorods, obtained through hydrothermal synthesis, were prepared with two model pharmaceutical molecules characterized by low and pH-dependent solubility: meloxicam, a non-steroidal anti-inflammatory drug, and bumetanide, a diuretic drug. Both hybrids were physically and chemically characterized through the combined use of X-ray powder diffraction, scanning electron microscopy with energy-dispersive spectroscopy, differential scanning calorimetry, and infrared spectroscopy measurements. Then, their dissolution profiles and hydrophilicity (contact angles) in different media as well as their solubility were determined and compared to the pure drugs. This hybrid system seems particularly suitable as a drug carrier for bumetanide, as it shows higher drug loading and good dissolution profiles, while is less suitable for meloxicam, an acid molecule.
... Since first introduced by Sekiguchi and Obi in 1961, solid dispersions (SDs) have been the most predominantly used solid-state modification technique, found to have significant commercial success [19][20][21]. Since the first FDA-approved SD, Cesamet ® in 1985 (Bausch Health Companies Inc., Laval, QB, Canada), over 30 amorphous solid dispersions of Class II and Class IV drugs are now currently marketed as oral dosage forms, signifying the importance of this technique [20][21][22]. ...
... While the commercial success of BCS Class II drugs is limited by their inherent l dissolution, Class IV drugs show permeation-limited absorption. Among the vario physical and chemical modification techniques available, SDs provide a wide range opportunities, as they offer greater flexibility in formulating oral drug delivery syste given the availability of various processing and excipient alternatives [19]. The ease preparation and regulatory compliance requirements of SDs in comparison with te niques such as those involving the formation of solvates, hydrates, salt formation, the clusion of polar or ionizable groups, and co-crystallisation makes them a more favoura approach [22,27,28]. ...
... While the commercial success of BCS Class II drugs is limited by their inherent low dissolution, Class IV drugs show permeation-limited absorption. Among the various physical and chemical modification techniques available, SDs provide a wide range of opportunities, as they offer greater flexibility in formulating oral drug delivery systems given the availability of various processing and excipient alternatives [19]. The ease of preparation and regulatory compliance requirements of SDs in comparison with techniques such as those involving the formation of solvates, hydrates, salt formation, the inclusion of polar or ionizable groups, and co-crystallisation makes them a more favourable approach [22,27,28]. ...
Crystalline carriers such as dextrose, sucrose, galactose, mannitol, sorbitol, and isomalt have been reported to increase the solubility, and dissolution rates of poorly soluble drugs when employed as carriers in solid dispersions (SDs). However, synthetic polymers dominate the preparation of drugs: excipient SDs have been created in recent years, but these polymer-based SDs exhibit the major drawback of recrystallisation upon storage. Also, the use of high-molecular-weight polymers with increased chain lengths brings forth problems such as increased viscosity and unnecessary bulkiness in the resulting dosage form. An ideal SD carrier should be hydrophilic, non-hygroscopic, have high hydrogen-bonding propensity, have a high glass transition temperature (Tg), and be safe to use. This review discusses sugars and polyols as suitable carriers for SDs, as they possess several ideal characteristics. Recently, the use of low-molecular-weight excipients has gained much interest in developing SDs. However, there are limited options available for safe, low molecular excipients, which opens the door again for sugars and polyols. The major points of this review focus on the successes and failures of employing sugars and polyols in the preparation of SDs in the past, recent advances, and potential future applications for the solubility enhancement of poorly water-soluble drugs.
... Therefore, numerous attempts have been made to improve the dissolution of certain drugs to obtain a more rapid and complete absorption. To this aim, salt formation, complexation, micelles, liposomes, particle size reduction, and solid dispersion were some of the contrived methods [2][3][4]. Lately, one of the most promising systems for the pharmaceutical industry that is attracting considerable attention is represented by inorganic-organic hybrids formed by a host inorganic matrix and a drug guest [5,6]. In this regard, hydroxyapatites and layered double hydroxides are certainly very interesting inorganic matrices. ...
... The most intense peaks are those of the basal diffraction of 00l reflections of LDHs, with the NO 3 − as intercalated anions, due to the employed reagents. The small peak near to the main reflection at about 10 • can suggest the intercalation of some CO 3 2− , notwithstanding the use of decarbonated solvents and N 2 flux during the synthesis. From the peak position of the 003 reflection (2θ = 10.1 • ) it is possible to calculate an interplanar distance of 8.75 Å, in agreement with literature data [17,31]. ...
... Additionally, the occurrence of bands at around 1400 cm −1 suggests that HAP is carbonated [33]. The inclusion of CO 3 2ions was due to the CO 2 present in the environment during the synthesis. It has been reported that carbonated HAP offered better bioactivity [33]. ...
The search for effective systems to facilitate the release of poorly bioavailable drugs is a forefront topic for the pharmaceutical market. Materials constituted by inorganic matrices and drugs represent one of the latest research strategies in the development of new drug alternatives. Our aim was to obtain hybrid nanocomposites of Tenoxicam, an insoluble nonsteroidal anti-inflammatory drug, with both layered double hydroxides (LDHs) and hydroxyapatite (HAP). The physicochemical characterization on the base of X-ray powder diffraction, SEM/EDS, DSC and FT-IR measurements was useful to verify the possible hybrids formation. In both cases, the hybrids formed, but it seemed that the drug intercalation in LDH was low and, in fact, the hybrid was not effective in improving the pharmacokinetic properties of the drug alone. On the contrary, the HAP-Tenoxicam hybrid, compared to the drug alone and to a simple physical mixture, showed an excellent improvement in wettability and solubility and a very significant increase in the release rate in all the tested biorelevant fluids. It delivers the entire daily dose of 20 mg in about 10 min.
... For this, the solid dispersion method is a useful, economical, and environmentally beneficial choice based on its combination with hydrophilic polymers. A solid dispersion system is defined as a solid-phase system in which one or more drugs are dispersed in one or more pharmacologically inert carriers [14,15]. Solid dispersion has been proven to significantly improve the solubility of poor soluble drugs such as azithromycin [16,17]. ...
... Solid dispersion has been proven to significantly improve the solubility of poor soluble drugs such as azithromycin [16,17]. Regarding the solid dispersion fabrication, two commonly utilized methods are the wet grinding method and the solvent evaporation method [18], which possess the advantages of less organic solvents and drug decomposition avoidance [14,19], and the homogenization of the drugs and the polymers [14,20], respectively. ...
... Solid dispersion has been proven to significantly improve the solubility of poor soluble drugs such as azithromycin [16,17]. Regarding the solid dispersion fabrication, two commonly utilized methods are the wet grinding method and the solvent evaporation method [18], which possess the advantages of less organic solvents and drug decomposition avoidance [14,19], and the homogenization of the drugs and the polymers [14,20], respectively. ...
Azithromycin, a macrolide antibiotics, is one of the frequently used drugs in the children and elder. However, due to these population difficulty in swallowing and inefficient absorption, and azithromycin inherent poor solubility, bitter taste, and instability in the stomach acidic condition, it is a challenge to reach high oral bioavailability of this drug. To overcome these issues, we developed and characterized the effervescent granules containing azithromycin solid dispersion. Firstly, the solid dispersion was prepared, employing both wet grinding and solvent evaporation methods, with different types/amounts of polymers. The optimal solid dispersion with β-cyclodextrin at a drug:polymer ratio of 1:2 (w/w), prepared by the solvent evaporation method, significantly enhanced the azithromycin solubility 4-fold compared to the free drug, improved its bitterness from “bitter” to “normal”, possessed intermolecular bonding between the drug and polymer, and transformed the azithromycin molecules from crystalline to amorphous state. Secondly, the effervescent granules incorporating the solid dispersion were formulated with varied excipients of sweeteners, gas-generators, pH modulators, and glidants/lubricants. The optimal formula satisfied all the properties stated in the Vietnamese Pharmacopoeia. In summary, the final effervescent granules product could be further investigated in in-vivo and in clinical settings to become a potential azithromycin delivery system with high bioavailability for the children and elder.
... Poor water solubility and/or poor membrane permeability of the drug molecule are the most important contributors to inadequate medication absorption from the gastrointestinal (GI) tract. When an active substance is administered orally, it must first dissolve in the stomach and/or intestines before it can pass through the gastrointestinal tract's membranes and enter the bloodstream 1 . As a result, a medicine with poor water solubility often exhibits restricted absorption by dissolving rate, while a drug with poor membrane permeability typically exhibits limited absorption by permeation rate. ...
Antipsychotic medication lurasidone is used to treat schizophrenia and bipolar disorder. In this study, a new effort was made to improve the solubility, rate of dissolution, and oral bioavailability of the poorly soluble drug lurasidone by manufacturing it as solid dispersions utilising a variety of methods and a carrier called polyethylene glycol (PEG) 6000. The prepared solid dispersions were used to prepare fast dissolving tablets by using super disintegrants. A novel super disintegrant called Microcrystalline Cellulose-Polyethylene Glycol (MCC-PEG) Conjugate was also created as part of the project. PEGylation of Microcrystalline Cellulose (MCC) was done since PEG has the ability to increase the water absorption capacity and MCC acts as a disintegrant. Super disintegrants such as sodium starch glycolate, croscarmellose sodium, crospovidone, and microcrystalline cellulose (MCC)-polyethylene glycol (PEG) conjugate were used to create Lurasidone tablets that dissolve quickly. Tablets were tested for physical parameters and drug release by in vitro dissolution studies. Through SEM examination, DSC, and XRD tests, optimised solid dispersions surface properties, drug-excipient interactions, and crystal morphology have all been assessed. All the tablet preparations containing superdisintegrants were formed to release the drug in the order MCC-PEG Conjugate>Crospovidone> Croscarmellose sodium > Sodium starch glycolate. The dissolution rate of such tablet formulations were found to release the drug at a faster rate than the tablets prepared with plain drug
... As a result, the drug's solubility was improved, resulting in better oral absorption. Hydrophilic carriers are critical for improving drug wettability and maintaining the super-saturable state [24][25][26][27][28]. Aceclofenac (AFC) (2-[(2,6-dichlorophenyl) amine] phenylacetoxyacetic acid) is a new generational non-steroidal anti-inflammatory drug (NSAID) that is thought to be a better option for diclofenac and other NSAIDs in term of gastrointestinal safety [29,30]. ...
The major objective of the current study is to implement a plan to enhance the dissolution rate and oral bioavailability of a poorly water-soluble aceclofenac. The drug is classified according to the biopharmaceutical classification system as class II drug. Amorphous alkalinized aceclofenac solid dispersion was formulated as a ternary mixture. This mixture was prepared by introducing polymeric carriers [polyvinylpyrrolidone, Hydroxy propyl beta cyclodextrin or Polyethylene glycol] and an alkalizer (Na2CO3) by applying the solvent evaporation method. Optimum formulations were compressed into tablets that were subjected to in-vitro studies compared to the market product Bristaflam and free drug containing one. Finally, tablets were assessed for stability studies and carrageenan-induced rat paw edema treatment to evaluate potentiated anti-inflammatory efficacy. Results showed that optimum amorphous alkalinized aceclofenac solid dispersion formulations containing polyvinylpyrrolidone K30 or Hydroxy propyl beta cyclodextrin in 1:5 ratio have significant in-vitro dissolution improvement (>90% in 10 min) compared to untreated aceclofenac. Solid-state characterization emphasized the conversion of the crystalline drug into the amorphous form with no drug−polymers interactions. Stability and dissolution studies ensured that tablets containing amorphous alkalinized solid dispersions were stable with strikingly improving dissolution behavior compared to Bristaflam or free drug containing tablets. Moreover, regarding anti-inflammatory activity against carrageenan induced paw edema, and histopathological examination, we concluded that amorphous alkalinized solid dispersions containing tablets are a promising approach to enhance the dissolution rate and oral bioavailability and hence anti-inflammatory efficacy of aceclofenac.
