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Polymers play vital role in drug delivery systems. Aim of current research work was to elucidate the effect of Hydroxyethyl cellulose (HEC), acrylic acid (AA) and N'N'-methylene bis-acrylamide (MBA) in formulation of pH sensitive nexus for targeted delivery of acid sensitive drug perindopril erbumine (PE). Different feed ratios were employed to pre...
Citations
... Ijaz and Tulain reported a similar phenomenon, stating that as MBA concentration increases, hydrogel swelling followed by drug release decreases. [51] SD3 and HA3 systems were selected as optimized formulations based on LST release. Figure 15 shows the response surface methodology (RSM) plot and contour plots of optimized IC3, SD3, and HA3 formulations. ...
Our study focused on developing and optimizing β-CD-based microparticulate carrier systems to enhance lovastatin's solubility and systemic availability (LST). Specifically, we designed solid dispersions, inclusion complexes, and hydrogel microparticles as carrier systems. Fourier-transform infrared spectroscopy (FTIR) studies were conducted to ensure drug-polymer interactions and ingredient compatibility. Additionally, we investigated the physical state, thermal stability, topology, internal morphology, and particle size using techniques such as powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), scanning electron microscopy (SEM), transmission electron microscopy (TEM), zeta size, and zeta potential. Our results confirmed the formation of compatible and thermally stable networks within an acceptable particle size range. The entrapment efficiency and product yield fell within 83.50-88.50% and 87-90.50%, respectively. Notably, all developed formulations exhibited a significant increase in solubility at pH 6.8 compared to LST commercial Tablets, as indicated by the regression coefficient (R2) for the release of LST following first-order kinetics. We compared LST commercial Tablets with our optimized formulations (SD3 and HA3) for pharmacokinetic evaluation. SD3 demonstrated a Cmax of 63.64 µg/ml, an AUC o-t of 555.79 µg/ml.hr, and a half-life (t1/2) of 7.3 hours. In contrast, HA3 exhibited superior pharmacokinetic parameters with a Cmax of 93.543 µg/ml, an AUC o-t of 1154.35 µg/ml.hr, and a t1/2 of 10.33 hours. These results indicate the efficient release of LST from the developed carrier systems, supported by increased Cmax and lower tmax values. Furthermore, biochemical and histopathological studies on our optimized formulations confirmed their biocompatibility. Our findings demonstrate our developed β-CD-based microparticulate carrier systems' effectiveness in enhancing lovastatin's solubility, systemic availability, and biocompatibility.
... It was observed that NGP6, which contained a higher concentration of MAA, exhibited a more increased swelling. Similar findings 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55 56 57 58 59 60 were reported by , who formulated an HEC-co-poly (AA)-based polymeric nexus for colon targeting of perindopril erbumine [39]. ...
The purpose current research is to formulate a smart drug delivery system for solubility enhancement and sustained release of hydrophobic drugs. Drug solubility-related challenges constitute a significant concern for formulation scientists. To address this issue, a recent study focused on developing PEG-g-poly (MAA) co-polymeric nanogels to enhance the solubility of Olmesartan, a poorly soluble drug. The researchers employed a free radical polymerization technique to formulate these nanogels. Nine formulations were formulated. The newly formulated nanogels underwent comprehensive tests, including physicochemical assessments, dissolution studies, solubility evaluations, toxicity investigations, and stability examinations. FTIR investigations confirmed the successful encapsulation of Olmesartan within the nanogels, while TGA and DSC studies verified their thermal stability. SEM images revealed the presence of pores on the surface of the nanogels, facilitating water penetration and promoting rapid drug release. Moreover, PXRD studies indicated that the prepared nanogels exhibited an amorphous structure. The nanogel carrier system led to a significant enhancement in olmesartan's solubility, achieving a remarkable 12.3-fold increase at pH 1.2 and 13.29-fold rise in phosphate buffer of pH 6.8 (NGP3). Significant swelling was observed at pH 6.8 as compared to pH 1.2. Moreover, formulated nexus is non-toxic and bio-compatible and depicted considerable potential for delivery of drugs, protein as well as heat sensitive active moieties.
... Peaks at 1602 cm −1 and 1242 cm −1 show the presence of C=O and C-N groups. Peaks at 2868 cm −1 and 1111 cm −1 were due to the C-H group and alkyl aryl ether linkage, respectively [35]. The FTIR spectrum of MAA indicated a peak at 2941 cm −1 that was due to asymmetric stretching of methyl C-H group. ...
... Peaks at 1602 cm −1 and 1242 cm −1 show the presence of C=O and C-N groups. Peaks at 2868 cm −1 and 1111 cm −1 were due to the C-H group and alkyl aryl ether linkage, respectively [35]. ...
... The presence of this porous structure in drug-loaded hydrogels is a critical aspect to consider. It is expected to have a significant impact on both the rate and extent of hydrogel swelling and, consequently, on drug release kinetics, as has been discussed in prior research [35]. 3.2.8. ...
Citation: Sarfraz, M.; Tulain, U.R.; Erum, A.; Malik, N.S.; Mahmood, A.; Sumaira; Aslam, S.; Sandhu, M.A.; Tayyab, M. Cydonia oblonga-Seed-Abstract: The primary objective of this study was to assess the potential utility of quince seed mucilage as an excipient within a graft copolymer for the development of an oral-controlled drug delivery system. The Cydonia oblonga-mucilage-based graft copolymer was synthesized via a free radical polymerization method, employing potassium per sulfate (KPS) as the initiator and N, N-methylene bisacrylamide (MBA) as the crosslinker. Various concentrations of monomers, namely acrylic acid (AA) and methacrylic acid (MAA), were used in the graft copolymerization process. Metoprolol tartarate was then incorporated into this graft copolymer matrix, and the resultant drug delivery system was subjected to comprehensive characterization using techniques such as Fourier-transform infrared spectroscopy (FTIR) and scanning electron microscopy (SEM). The swelling behavior of the drug delivery system was evaluated under different pH conditions, and in vitro drug release studies were conducted. Furthermore, pharmacokinetic parameters including the area under the curve (AUC), maximum plasma concentration (Cmax), time to reach Cmax (Tmax), and half-life (t1/2) were determined for metoprolol-loaded hydrogel formulations in rabbit plasma, and these results were compared with those obtained from a commercially available product. The key findings from the study include observations that higher concentrations of acrylic acid (AA) and Cydonia oblonga mucilage (CM) in the graft copolymer enhanced swelling, while the opposite trend was noted at elevated concentrations of methacrylic acid (MAA) and N, N-methylene bisacrylamide (MBA). FTIR analysis confirmed the formation of the graft copolymer and established the compatibility between the drug and the polymer. SEM imaging revealed a porous structure in the prepared formulations. Additionally, the swelling behavior and drug release profiles indicated a pH-sensitive pattern. The pharmacokinetic assessment revealed sustained release patterns of metoprolol from the hydrogel network system. Notably, the drug-loaded formulation exhibited a higher Cmax (156.48 ng/mL) compared to the marketed metoprolol product (96 ng/mL), and the AUC of the hydrogel-loaded metoprolol was 2.3 times greater than that of the marketed formulation. In conclusion, this study underscores the potential of quince seed mucilage as an intelligent material for graft-copolymer-based oral-controlled release drug delivery systems.
... It has a chain structure in which anhydrous glucose units are attached to each other by β-1,4linkage giving rise to three free hydroxyl groups in each unit. These free hydroxyl groups make it a suitable polymer for hydrogel fabrication [50]. ...
... It is comprised of L-rhamnose, D-galactose, and L-galacturonic acid in its composition (Figure 12) [76]. In pharmaceutical industry, although its role has not been explored enough as hydrogel preparations, it is evaluated as an economical and effective binding agent in solid dosage forms [45,47,48], in forming controlled release matrices [49,50], for preparation of sustained release beads [51], microspheres [52,53], in mucoadhesive nasal gel [54] and in many other formulations as a sustained release polymer. ...
This book chapter give an overview of natural and synthetic polymeric moieties consumed for developing hydrogels and their types. Different properties of nanogels are the advancement of hydrogels characterized by nano-size range, stimuli-responsive swelling, and release. Stimuli responsiveness is imparted by the presence of a suitable monomer. A number of polymerization approaches are presented in the literature that are employed to prepare such networks. These systems are elastic, rubbery, nontoxic, and biocompatible and offer prolonged release of the drugs without chances of dose dumping. These types of networks have potential pharmaceutical, agricultural, food, and biotechnological applications in terms of controlled, prolonged, and targeted drug delivery, solubility enhancements, stimuli-dependent intelligent drug delivery, such as contact lenses, wound healing, etc. In the current chapter, we have tried to introduce hydrogels and microgels, their different types, the variety of polymers used to develop such carrier systems, approaches to develop such drug delivery systems, and their utilization in various sectors in addition to the pharmaceutical sector.
... These findings are in line with the results reported by Ijaz et al. (2018), who developed IPNs containing Natrosol and Acrylic Acid for controlled delivery of Perindopril Erbumine and observed similar results. Ijaz and Tulain, (2019) observed similar findings that when the percentage of HEC was increased from 2-4%, swelling was also promoted from 53.76-55.41% at alkaline pH. ...
Background & objectives:
This study aimed to create a controlled delivery system for Tapentadol Hydrochloride by developing interpenetrating networks (IPNs) of Natrosol-Pectin copolymerized with Acrylic Acid and Methylene bisacrylamide, and to analyze the effects of various ingredients on the physical and chemical characteristics of the IPNs.
Methods:
Novel Tapentadol Hydrochloride-loaded Natrosol-Pectin based IPNs were formulated by using the free radical polymerization technique. Co-polymerization of Acrylic Acid (AA) with Natrosol and Pectin was performed by using Methylene bisacrylamide (MBA). Ammonium persulfate (APS) was used as the initiator of crosslinking process. The impact of ingredients i.e. Natrosol, Pectin, MBA, and Acrylic Acid on the gel fraction, porosity, swelling (%), drug loading, and drug release was investigated. FTIR, DSC, TGA, SEM and EDX studies were conducted to confirm the grafting of polymers and to evaluate the thermal stability and surface morphology of the developed IPNs.
Results:
Swelling studies exhibited an increase in swelling percentage from 84.27 to 91.17% upon increasing polymer (Natrosol and Pectin) contents. An increase in MBA contents resulted in a decrease in swelling from 85 to 67.63%. Moreover, the swelling was also observed to increase with higher AA contents. Significant drug release was noted at higher pH instead of gastric pH value. Oral toxicological studies revealed the nontoxic and biocompatible nature of Natrosol-Pectin IPNs.
Interpretation & conclusion:
The developed IPNs were found to be an excellent system for the controlled delivery of Tapentadol Hydrochloride.
... However, when hydrogels were dipped in simulated intestinal pH, a dramatic surge in swelling ratio was witnessed as shown in Figure 2. This was due to the pH of the surrounding medium, which was above the pKa of AA (4.28) [41]. At this pH, carboxylic groups are easily deprotonated, which results in an increase in electrostatic repulsion and swelling of polymeric network. ...
In this paper, we fabricated semi-interpenetrating polymeric network (semi-IPN) of hydroxypropyl-β-cyclodextrin-grafted-poly(acrylic acid)/poly(vinyl pyrrolidone) (HP-β-CD-g-poly(AA)/PVP) by the free radical polymerization technique, intended for colon specific release of dexamethasone sodium phosphate (DSP). Different proportions of polyvinyl pyrrolidone (PVP), acrylic acid (AA), and hydroxypropyl-beta-cyclodextrin (HP-β-CD) were reacted along with ammonium persulphate (APS) as initiator and methylene-bis-acrylamide (MBA) as crosslinker to develop a hydrogel system with optimum swelling at distal intestinal pH. Initially, all formulations were screened for swelling behavior and AP-8 was chosen as optimum formulation. This formulation was capable of releasing a small amount of drug at acidic pH (1.2), while a maximum amount of drug was released at colonic pH (7.4) by the non-Fickian diffusion mechanism. Fourier transformed infrared spectroscopy (FTIR) revealed successful grafting of components and development of semi-IPN structure without any interaction with DSP. Thermogravimetric analysis (TGA) confirmed the thermal stability of developed semi-IPN. X-ray diffraction (XRD) revealed reduction in crystallinity of DSP upon loading in the hydrogel. The scanning electron microscopic (SEM) images revealed a rough and porous hydrogel surface. The toxicological evaluation of semi-IPN hydrogels confirmed their bio-safety and hemocompatibility. Therefore, the prepared hydrogels were pH sensitive, biocompatible, showed good swelling, mechanical properties, and were efficient in releasing the drug in the colonic environment. Therefore, AP-8 can be deemed as a potential carrier for targeted delivery of DSP to treat inflammatory bowel diseases.
... Drug loading was estimated by weight method, swelling method and extraction method. By weight method, the difference in the initial and the final weight was calculated [12][13][14][15] : ...
... Pressure was applied which results in formation of dense mass. FTIR studies were conducted at range of 3500-600 cm À1 [15] . ...
... 3. Thermal analysis (differential scanning calorimetry and thermogravimetric analysis) DSC and TGA of chitosan, MBA, potassium persulfate, acrylic acid, unloaded and drug loaded hydrogel was conducted by employing TA (analysis) system Q2000 at 30-400 C [15] . ...
... pH responsive behavior is attributed to crosslinking of pectin with acrylates by employing N,N-methylene bisacrylamide (MBA) as branched crosslinker thereby imparting mechanical strength to 3-D architecture. Few reports have been reported on investigation of pectin application for fascinating colon targeting [8,9,10,11]. ...
... The results are shown in Figs. 4,5,6,7,8,9,10,11,12,13,14,15 , 16 and 17 and Tables 2, 3, 4, 5, 6 and 7. ...
... Furthermore, decrease in crystallinity aids in swelling of formulated nexus. Moreover, Ijaz and his coworkers reported to reduce crystallinity in formulated nexus which claims amorphous nature of fabricated nexus [9]. ...
In current research work, pH responsive pectin-co-poly(MAA) hydrogels containing diloxanide furoate were developed by graft polymerization of pectin and methacrylic acid, for the treatment of amebiasis. Developed hydrogels were evaluated
for drug loading efciency, swelling behavior, porosity, sol–gel fraction and drug
release kinetics. Ex vivo mucoadhesion, X-ray and acute oral toxicity studies were
also conducted. Structural entanglement was revealed by FTIR spectroscopy. Differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA) evaluation exhibited better thermal stability of developed hydrogel. The optimized
hydrogel (PM6) showed pH responsiveness by providing maximum swelling of
95.16±0.054% in alkaline media (pH 7.4), and 91.37±0.53% drug release occurs
in pH 7.4 up to 24 h. Scanning electron microscopy (SEM) revealed the presence
of tiny channels in the network which signifcantly promote swelling of developed
hydrogel. In vivo gastrointestinal transit behavior of optimized formulation (PM-6)
was evaluated by X-ray imaging on albino rabbits. Acute oral toxicity studies after
administered of developed hydrogel indicated no signs of histopathology or any dermal toxicity. Hence, current investigation suggests that PM6 could be a promising
approach for colon delivery. Thus, the proposed work would be helpful for the treatment of amebiasis
... Many polymers and copolymers are produced from these reactions which impart mechanical strength and toughness to the formed polymer. It maintains the gel structure and keeps it firm as it forms network when crosslinks with polyacrylamides rather than forming linear chains [16][17][18]. ...
... Young's modulus was determined taking slope from tensile stress-strain curve. Similarly, stress (σ), i.e., force per unit area, and strain (ε), i.e., change in length, were determined by using the following expressions: where F = actual force applied, r = hydrogel radius and where li = initial length of hydrogel and If = final length of hydrogel [16]. ...
... Discs were weighed again when excess of ethanol was seen on the surface. Percentage porosity was then computed by using formula [16]. ...
The aim of the current research work was to fabricate polymeric nexus for controlled delivery of metoprolol tartrate by using free radical polymerization. Polymer (aloe vera, sodium carboxymethyl cellulose, and meggletose) was crosslinked with monomer (acrylic acid) by using N,N methylene bisacrylamide. Swelling behavior was studied in pH 1.2 and 7.4. Sol gel fraction depicted gel fraction increased with the increase in feed ratio (polymer, monomer, and crosslinker). Optimized formulation was evaluated via Fourier transform infrared spectroscopy (FTIR) and scanning electron microscopy (SEM). FTIR confirmed compatibility of metoprolol with formulated system. Moreover, pH-dependent swelling was observed, experiencing significant swelling at higher pH. SEM depicted porous architecture which is responsible for swelling, drug loading, and release. Dissolution studies showed percentage drug release was significant in pH 7.4. Hence, the current research work demonstrates sustained delivery of metoprolol by employing varying concentration of polymer, monomer, and crosslinker. These fascinating properties made hydrogel a promising carrier for sustained drug delivery.
Graphic abstract
... Drug loading was estimated by weight method, swelling method and extraction method. By weight method, the difference in the initial and the final weight was calculated [12][13][14][15] : ...
... Pressure was applied which results in formation of dense mass. FTIR studies were conducted at range of 3500-600 cm À1 [15] . ...
... 3. Thermal analysis (differential scanning calorimetry and thermogravimetric analysis) DSC and TGA of chitosan, MBA, potassium persulfate, acrylic acid, unloaded and drug loaded hydrogel was conducted by employing TA (analysis) system Q2000 at 30-400 C [15] . ...
In current research study, novel chitosan-based hydrogel was formulated via crosslinking graft copolymerization of acrylic acid (AA) and chitosan. Potassium persulfate was used as free radical generator in the presence of crosslinker (methylene bis acrylamide (MBA)). FTIR spectroscopy was employed to elucidate structure of hydrogel. Moreover, sample morphology was examined by scanning electron microscopy (SEM) and thermal analysis was conducted by using thermogravimetric analysis (DSC/TGA). The influence of reaction variables such as concentration of chitosan (CS), acrylic acid (AA) and MBA was optimized to attain hydrogel with significant swelling capacity. Chitosan-g-AA hydrogel depicted pH responsive attributes and swelling–deswelling pulsatile behavior was recorded at pHs 1.2 and 7.4. This on–off switching makes hydrogel ideal candidate for controlled drug delivery.
