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3.
Pharmaceutics ; 16(1)2024 Jan 22.
Article En | MEDLINE | ID: mdl-38276522

The journal retracts the article, "Poly (N-vinylcaprolactam-grafted-sodium alginate) Based Injectable pH/Thermo Responsive In Situ Forming Depot Hy-drogels for Prolonged Controlled Anticancer Drug Delivery; In Vitro, In Vivo Characterization and Toxicity Evaluation" [...].

4.
Curr Pharm Des ; 29(31): 2489-2500, 2023.
Article En | MEDLINE | ID: mdl-37881070

BACKGROUND: Diclofenac sodium has a short half-life (about 1.5 hours), requiring repeated administration, and as a result, serious complications, such as GI bleeding, peptic ulcer, and kidney and liver dysfunction, are generated. Hence, a sustained/controlled drug delivery system is needed to overcome the complications caused by the administration of diclofenac sodium. AIMS: This study aimed to fabricate and evaluate carbopol/polyvinyl alcohol-based pH-sensitive hydrogels for controlled drug delivery. OBJECTIVE: pH-sensitive carbopol/polyvinyl alcohol graft-poly(acrylic acid) hydrogels (Cp/PVA-g-PAa hydrogels) were developed for the controlled delivery of diclofenac sodium. METHODS: The combination of carbopol/polyvinyl alcohol, acrylic acid, and ethylene glycol dimethacrylate was used as polymer, monomer, and cross-linker, respectively. The effects of the formulation's composition on porosity, swelling index, and release pattern of diclofenac sodium from the developed hydrogels were investigated. RESULTS: An increase in porosity and swelling was observed with the increasing amounts of carbopol and acrylic acid, whereas polyvinyl alcohol showed the opposite effect. Due to the formation of a highly viscous system, the drug release decreased with the increasing concentrations of carbopol and polyvinyl alcohol while increased with increasing acrylic acid concentration. The pH-responsive properties of the fabricated hydrogels were demonstrated by dynamic swelling and drug release studies at three different pH values. Higher dynamic swelling and diclofenac sodium (model drug) release were found at high pH values compared to low pH values, i.e., pH 7.4 > 4.6 > 1.2, respectively. Cytotoxicity studies reported no toxic effect of the prepared hydrogels, thus indicating that the prepared hydrogels are safe to be used on clinical basis. CONCLUSION: The prepared carbopol/polyvinyl alcohol crosslinked hydrogel can be used as a promising carrier for the controlled release of drugs.


Diclofenac , Polyvinyl Alcohol , Humans , Polyvinyl Alcohol/chemistry , Polyvinyl Alcohol/pharmacology , Cross-Linking Reagents/chemistry , Cross-Linking Reagents/pharmacology , Drug Delivery Systems , Hydrogels/chemistry , Hydrogen-Ion Concentration , Drug Liberation
5.
Int J Biol Macromol ; 252: 126464, 2023 Dec 01.
Article En | MEDLINE | ID: mdl-37619682

Current study reports the combined technique of microneedle array patches and thermoresponsive gels. Microneedles array patch mediated insitu skin depots were evaluated for sustain drug delivery using sodium alginate/Poly (vinylcaprolactam) thermoresponsive gels. Their phase transition property from sol-gel state was monitored with AR2000 rheometer. Ibuprofen sodium was loaded in optimized formulations. The non-soluble cross-linked microneedle array patches (MAPs) were prepared from variable biocompatible polymers using silicone micromoulds. The fabricated MAPs were evaluated for mechanical stability, inskin dissolution, insertion forces and moisture contents. The penetration depth of MAPs in neonatal rabbit skin was tracked by optical coherence tomography. The optimized MAPs (GP10000) were used as microporation source in skin owing to their stable nature. Pores formation in skin samples after MAPs treatment was confirmed by optical coherence tomography, dye binding and skin integrity analysis. The invitro permeation of Ibuprofen sodium from formulations was studied using Franz cells across intact skin and MAPs applied skin. It was concluded from the results that Ibuprofen sodium permeation was observed for longer time through MAPs treated skin as compared to intact skin. Confocal study confirmed the diffusion of drug loaded formulations in deeper tissues with higher intensity.


Alginates , Ibuprofen , Animals , Rabbits , Ibuprofen/pharmacology , Alginates/chemistry , Administration, Cutaneous , Drug Delivery Systems/methods , Gels , Sodium , Transdermal Patch
6.
Int J Biol Macromol ; 251: 126380, 2023 Aug 16.
Article En | MEDLINE | ID: mdl-37595715

Bone tissue possesses intrinsic regenerative capabilities to address deformities; however, its ability to repair defects caused by severe fractures, tumor resections, osteoporosis, joint arthroplasties, and surgical reconsiderations can be hindered. To address this limitation, bone tissue engineering has emerged as a promising approach for bone repair and regeneration, particularly for large-scale bone defects. In this study, an injectable hydrogel based on kappa-carrageenan-co-N-isopropyl acrylamide (κC-co-NIPAAM) was synthesized using free radical polymerization and the antisolvent evaporation technique. The κC-co-NIPAAM hydrogel's cross-linked structure was confirmed using Fourier transform infrared spectra (FTIR) and nuclear magnetic resonance (1H NMR). The hydrogel's thermal stability and morphological behavior were assessed using thermogravimetric analysis (TGA) and scanning electron microscopy (SEM), respectively. Swelling and in vitro drug release studies were conducted at varying pH and temperatures, with minimal swelling and release observed at low pH (1.2) and 25 °C, while maximum swelling and release occurred at pH 7.4 and 37oC. Cytocompatibility analysis revealed that the κC-co-NIPAAM hydrogels were biocompatible, and hematoxylin and eosin (H&E) staining demonstrated their potential for tissue regeneration and enhanced bone repair compared to other experimental groups. Notably, digital x-ray examination using an in vivo bone defect model showed that the κC-co-NIPAAM hydrogel significantly improved bone regeneration, making it a promising candidate for bone defects.

7.
Int J Pharm ; 643: 123244, 2023 Aug 25.
Article En | MEDLINE | ID: mdl-37463619

The study aims to develop a new multifunctional biopolymer-based hydrogel membrane dressing by adopting a solvent casting method for the controlled release of cefotaxime sodium at the wound site. Sodium alginate enhances collagen production in the skin, which provides tensile strength to healing tissue. Moreover, the significance of extracellular molecules such as hyaluronic acid in the wound the healing cascade renders these biopolymers an essential ingredient for the fabrication of hydrogel membranes via physical crosslinking (hydrogen bonding). These membranes were further investigated in terms of their structure, and surface morphology, as well as cell viability analysis. A membrane with the most suitable characteristics was chosen as a candidate for cefotaxime sodium loading and in vivo analysis. Results show that the 3D porous nature of developed membranes allows optimum water vapor and oxygen transmission (>8.21 mg/mL) to divert excessive wound exudate away from the diabetic wound bed, MTT assay confirmed cell viability at more than 80%. In vivo results confirmed that the CTX-HA-Alg-PVA hydrogel group showed rapid wound healing with accelerated re-epithelization and a decreased inflammatory response. Conclusively, these findings indicate that CTX-HA-Alg-PVA hydrogel membranes exhibit a suitable niche for use as dressing membranes for healing of diabetic wounds.


Diabetes Mellitus , Hydrogels , Humans , Hydrogels/chemistry , Hyaluronic Acid/chemistry , Alginates , Biomimetics , Wound Healing , Cefotaxime
8.
Int J Biol Macromol ; 233: 123585, 2023 Apr 01.
Article En | MEDLINE | ID: mdl-36758757

The disease-related suffering in colorectal cancer remains prevalent despite advancements in the field of drug delivery. Chemotherapy-related side effects and non-specificity remain a challenge in drug delivery. The great majority of hydrophobic drugs cannot be successfully delivered to the colon orally mainly due to poor solubility, low bioavailability, pH differences, and food interactions. Polymeric nanoparticles are potential drug delivery candidates but there are numerous limitations to their usefulness in colon cancer. The nanoparticles are removed from the body rapidly by p-glycoprotein efflux, inactivation, or breakdown by enzymes limiting their efficiency. Furthermore, there is a lack of selectivity in targeting cancer cells; nanoparticles may also target healthy cells, resulting in toxicity and adverse effects. The study aimed to use nanoparticles for specific targeting of the colorectal tumor cells via the oral route of administration without adverse effects. Folic acid (FA), a cancer-targeting ligand possessing a high affinity for folate receptors overexpressed in colorectal cancers was conjugated to sodium alginate- nanoparticles by NH2-linkage. The folic-acid conjugated nanoparticles (FNPs) were delivered to the colon by a pH-sensitive hydrogel synthesized by the free radical polymerization method to provide sustained drug release. The developed system referred to as the "Hydrogel-Nano (HN) drug delivery system," was specifically capable of delivering diferourylmethane to the colon. The HN system was characterized by DLS, FTIR, XRD, TGA, DSC, and SEM. The FNPs size, polydispersity index, and zeta potential were measured. The folic acid-conjugation to nanoparticles' surface was studied by UV-visible spectroscopy using Beer-Lambert's law. In-vitro studies, including sol-gel, porosity, drug loading, entrapment efficiency, etc., revealed promising results. The swelling and release studies showed pH-dependent release of the drug in colonic pH 7.4. Cellular uptake and cytotoxicity studies performed on FR-overexpressed Hela cell lines and FR-negative A-549 cell lines showed facilitated uptake of nanoparticles by folate receptors. A threefold increase in Cmax and prolongation of the mean residence time (MRT) to 14.52 +/- 0.217 h indicated sustained drug release by the HN system. The findings of the study can provide a sufficient ground that the synergistic approach of the HN system can deliver hydrophobic drugs to colorectal cancer cells via the oral route, but further in-vivo animal cancer model studies are required.


Colorectal Neoplasms , Nanoparticles , Humans , Animals , HeLa Cells , Folic Acid/chemistry , Hydrogels , Alginates , Drug Delivery Systems/methods , Colorectal Neoplasms/drug therapy , Nanoparticles/chemistry , Drug Carriers/chemistry
9.
Pharmaceutics ; 14(12)2022 Dec 15.
Article En | MEDLINE | ID: mdl-36559310

Microneedles are minimally invasive systems that can deliver drugs intradermally without pain and bleeding and can advantageously replace the hypodermal needles and oral routes of delivery. Deferasirox (DFS) is an iron chelator employed in several ailments where iron overload plays an important role in disease manifestation. In this study, DFS was formulated into a nanosuspension (NSs) through wet media milling employing PVA as a stabilizer and successfully loaded in polymeric dissolving microneedles (DMNs). The release studies for DFS-NS clearly showed a threefold increased dissolution rate compared to pure DFS. The mechanical characterization of DFS-NS-DMNs revealed that the system was sufficiently strong for efficacious skin penetration. Optical coherence tomography images confirmed an insertion of up to 378 µm into full-thickness porcine skin layers. The skin deposition studies showed 60% drug deposition from NS-DMN, which was much higher than from the DFS-NS transdermal patch (DFS-NS-TP) (without needles) or pure DFS-DMNs. Moreover, DFS-NS without DMNs did not deposit well inside the skin, indicating that DMNs played an important role in effectively delivering drugs inside the skin. Therefore, it is evident from the findings that loading DFS-NS into novel DMN devices can effectively deliver DFS transdermally.

10.
J Funct Biomater ; 13(4)2022 Dec 12.
Article En | MEDLINE | ID: mdl-36547555

The objective of the current study was to synthesize and characterize carbopol containing hydrogels with different monomers such as methacrylic acid (MAA), 2-acrylamido-2-methylpropane sulfonic acid (AMPS) and itaconic acid (ITA). Free radical polymerization method was optimized for the preparation of different formulations using N,N-methylene bis-acrylamide (MBA) as cross linking agent. Different studies were performed to evaluate the effect of different monomers on swelling, drug loading and drug release. Itopride Hydrochloride was used as model drug. FTIR, TGA, DSC and SEM were performed to probe the characteristics of fabricated hydrogels. Swelling studies of different fabricated hydrogels were performed in three pH conditions (1.2, 4.5 & 6.8). Higher swelling was observed at pH 6.8. An in-vitro release study was performed on pH 1.2 and 6.8. The synthesized hydrogels exhibited excellent mechanical strength, higher drug loading, pH sensitive and time dependent release up to 30 h. The excellent mechanical strength and extended drug release of Carbopol-co-poly-MAA-ITA hydrogels make them a potential candidate for controlled delivery of Itopride hydrochloride.

11.
Biomed Res Int ; 2022: 5883239, 2022.
Article En | MEDLINE | ID: mdl-36060130

Poor solubility is a global issue of copious pharmaceutical industries as large number of drugs in development stage as well as already marketed products are poorly soluble which results in low dissolution and ultimately dosage increase. Current study is aimed at developing a polyvinylpyrrolidone- (PVP-K30-) based nanogel delivery system for solubility enhancement of poorly soluble drug olanzapine (OLP), as solubilization enhancement is the most noteworthy application of nanosystems. Crosslinking polymerization with subsequent condensation technique was used for the synthesis of nanogels, a highly responsive polymeric networks in drug's solubility. Developed nanogels were characterized by percent entrapment efficiency, sol-gel, percent swelling, percent drug loaded content (%DLC), percent porosity, stability, solubility, in vitro dissolution studies, FTIR, XRD, and SEM analysis. Furthermore, cytotoxicity study was conducted on rabbits to check the biocompatibility of the system. Particle size of nanogels was found with 178.99 ± 15.32 nm, and in vitro dissolution study exhibited that drug release properties were considerably enhanced as compared to the marketed formulation OLANZIA. The solubility studies indicated that solubility of OLP was noticeably improved up to 36.7-fold in phosphate buffer of pH 6.8. In vivo cytotoxicity study indicated that prepared PVP-K30-based formulation was biocompatible. On the basis of results obtained, the developed PVP-K30-co-poly (AMPS) nanogel delivery system is expected to be safe, effective, and cost-effective for solubility improvement of poorly soluble drugs.


Polymers , Povidone , Animals , Drug Liberation , Nanogels , Polymers/chemistry , Povidone/chemistry , Rabbits , Solubility
12.
Pharmaceutics ; 14(9)2022 Sep 03.
Article En | MEDLINE | ID: mdl-36145612

The aim of the current investigation was based on the development of pH-responsive hydrogels of chondroitin sulfate, carbopol, and polyvinyl alcohol polymerized with acrylic acid in the presence of ammonium persulfate and ethylene glycol dimethylacrylate for controlled drug delivery. A free radical polymerization technique was used for the preparation of these pH-responsive hydrogels. The gel fraction of the prepared hydrogels was increased with the increase in the chondroitin sulfate, carbopol, polyvinyl alcohol, and acrylic acid content, while the sol-fraction was decreased. Swelling and drug release studies were performed in various pH conditions. Greater swelling and drug release were observed at high pH values (pH 4.6 and 7.4) as compared to low pH value (pH 1.2), representing the pH-responsive nature of the synthesized hydrogels. Porosity and drug loading were increased with the incorporation of high concentrations of hydrogel contents except polyvinyl alcohol, which showed reverse effects. Similarly, biodegradation study reported a slow degradation rate of the prepared hydrogels with the increase in hydrogel constituents. Cytotoxicity study proved the safe use of developed hydrogels as no toxic effect was shown on T84 human colon cancer cells. Similarly, various characterizations, including Fourier transform infrared spectroscopy, thermogravimetric analysis, differential scanning calorimetry, X-ray diffraction, and scanning electron microscopy, were performed for prepared hydrogels. Hence, we could demonstrate that the prepared hydrogels can be used as a promising drug carrier for the controlled delivery of drugs.

13.
Biomed Res Int ; 2022: 2426960, 2022.
Article En | MEDLINE | ID: mdl-35909483

Herein, we report nanogels comprising diverse feed ratio of polymer hydroxypropyl methylcellulose (HPMC), monomer acrylic acid (AA), and cross-linker methylene bisacrylamide (MBA) fabricated for transdermal delivery of finasteride (FIN). Free radical solution polymerization method with subsequent condensation was employed for the synthesis using ammonium per sulfate (APS) and sodium hydrogen sulfite (SHS) as initiators. Carbopol-940 gel (CG) was formulated as assisting platform to deliver FIN nanogels transdermally. Developed formulations were evaluated by several in vitro, ex vivo, and in vivo parameters such as particle size and charge distribution analysis, Fourier transform infrared spectroscopy (FTIR), thermogravimetric analysis (TGA), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), X-ray diffractogram (XRD), rheological testing, in vitro swelling and drug release, and ex vivo skin permeation, irritation, and toxicity assessment. The results endorsed the nanogel formation (117.3 ± 29.113 nm), and the impact of synthesizing method was signified by high yield of nanogels (≈91%). Efficient response for in vitro swelling and FIN release was revealed at pH 5.5 and 7.4. Skin irritation and toxicity assessment ensured the biocompatibility of prepared nanocomposites. On the basis of the results obtained, it can be concluded that the developed nanogels were stable with excellent drug permeation profile across skin.


Finasteride , Administration, Cutaneous , Drug Liberation , Finasteride/pharmacology , Hypromellose Derivatives , Nanogels , Spectroscopy, Fourier Transform Infrared
14.
Drug Dev Ind Pharm ; 48(6): 265-278, 2022 Jun.
Article En | MEDLINE | ID: mdl-35899871

Skin is considered as an attractive route for variety of drug molecule administration. However, it is proved to be the main physical barrier for drug flux owing to their poor permeability and low bioavailability across stratum corneum layer. In the current study, novel approach has been used to enhance transdermal delivery via microporation through combination of poloxamers gels and microneedles (MNs) arrays. The phase transition of poloxamers at various concentrations from sol-gel was evaluated using AR2000 rheometer to confirm MNs-assisted in situ forming depots. Temperature test confirmed gelation between 32 and 37 °C. Curcumin was loaded in poloxamer formulations at variable concentrations and its effect showed reduction in critical gelation temperature (CGT) owing to its hydrophobic nature. Microneedle arrays (600 µm) prepared from Gantrez S-97, PEG10000 and gelatin B using (19 × 19) laser-engineered silicone micromoulds showed high mechanical stability investigated via Texture analyzer. From in situ dissolution profile, gelatin 15% w/w based MNs displayed quicker dissolution rate in comparison to PG10000. VivoSight® OCT scanner and dye tracking confirmed that PG10000 MNs arrays pierced SC layer, infiltrate the epidermis and goes to dermis layer. From in vitro permeation, it was concluded that 20% w/w PF127® gel formulations containing (0.1% and 0.3%) curcumin displayed high curcumin permeation for comparatively longer time through microporated skin samples in comparison to non-microporated skin. The curcumin distribution in skin tissues with higher florescence intensity was noted in MNs treated skin samples by confocal microscopy. FTIR confirmed the structure formation of fabricated MNs, while TGA showed dry, brittle and rigid nature of gelatin MNs.


Curcumin , Poloxamer , Administration, Cutaneous , Drug Delivery Systems , Gelatin , Gels , Microinjections , Needles , Poloxamer/chemistry , Skin
15.
Int J Biol Macromol ; 215: 579-595, 2022 Aug 31.
Article En | MEDLINE | ID: mdl-35779651

The biopolymers-based two-fold system could provide a sustained release platform for drug delivery to the brain resisting the mucociliary clearance, enzymatic degradation, bypassing the first-pass hepatic metabolism, and BBB thus providing superior bioavailability through intranasal administration. In this study, poloxamers PF-127/PF-68 grafted chitosan HCl-co-guar gum-based thermoresponsive hydrogel loaded with eletriptan hydrobromide laden pullulan nanoparticles was synthesized and subjected to dynamic light scattering, Fourier transform infrared spectroscopy, thermal analysis, x-ray diffraction, scanning electron microscopy, stability studies, mucoadhesive strength and time, gel strength, cloud point assessment, rheological assessment, ex-vivo permeation, cell viability assay, histology studies, and in-vivo Pharmacokinetics studies, etc. It is quite evident that CSG-EH-NPs T-Hgel has an enhanced sustained release drug profile where approximately 86 % and 84 % of drug released in phosphate buffer saline and simulated nasal fluid respectively throughout 48 h compared to EH-NPs where 99.44 % and 97.53 % of the drug was released in PBS and SNF for 8 h. In-vivo PKa parameters i.e., mean residence time (MRT) of 11.9 ± 0.83 compared to EH-NPs MRT of 10.2 ± 0.92 and area under the curve (AUCtot) of 42,540.5 ± 5314.14 comparing to AUCtot of EH-NPs 38,026 ± 6343.1 also establish the superiority of CSG-EH-NPs T-Hgel.


Chitosan , Nanoparticles , Brain/metabolism , Chitosan/chemistry , Delayed-Action Preparations , Drug Carriers/chemistry , Drug Delivery Systems , Drug Liberation , Galactans , Glucans , Hydrogels/chemistry , Mannans , Nanoparticles/chemistry , Plant Gums
16.
Pharmaceutics ; 14(5)2022 May 13.
Article En | MEDLINE | ID: mdl-35631636

This study was aimed to develop novel in situ forming gels based on N-vinylcaprolactam, sodium alginate, and N,N-methylenebisacrylamide. The in situ Poly (NVRCL-g-NaAlg) gels were developed using the cold and free radical polymerization method. The structure formation, thermal stability, and porous nature of gels was confirmed by FTIR, NMR, DSC, TGA, and SEM. The tunable gelation temperature was evaluated by tube titling and rheological analysis. Optical transmittance showed that all formulations demonstrated phase transition around 33 °C. The swelling and release profile showed that gels offered maximum swelling and controlled 5-FU release at 25 °C and pH (7.4), owing to a relaxed state. Porosity and mesh size showed an effect on swelling and drug release. The in vitro degradation profile demonstrated a controlled degradation rate. An MTT assay confirmed that formulations are safe tested against Vero cells. In vitro cytotoxicity showed that 5-FU loaded gels have controlled cytotoxic potential against HeLa and MCF-7 cells (IC50 = 39.91 µg/mL and 46.82 µg/mL) compared to free 5-FU (IC50 = 50.52 µg/mL and 53.58 µg/mL). Histopathological study demonstrated no harmful effects of gels on major organs. The in vivo bioavailability in rabbits showed a controlled release in gel form (Cmax, 1433.59 ± 45.09 ng/mL) compared to a free drug (Cmax, 2263.31 ± 13.36 ng/mL) after the subcutaneous injection.

17.
Int J Biol Macromol ; 211: 425-440, 2022 Jun 30.
Article En | MEDLINE | ID: mdl-35577197

In current study, novel in situ formed injectable self-assembled thermoreversible depot gels based on N-(Vinylcaprolactam) were synthesized with a carbohydrate polymer i.e. sodium alginate in aqueous solution using cold method. The prepared gels preparations were intended to be utilized as 5-FU delivery depot after injectable administration through subcutaneous route. The structural characterization of self-assembled gels samples were studied through FTIR. The thermal properties of newly formed gels complexes were investigated by DSC and TGA. While the morphology of gels were assessed through SEM. The tunable gelation temperatures and phase transition of optimized formulations were confirmed by tube inverting, rheology determination and optical transmittance test. Thermo and pH response was evaluated at different temperatures and in various acidic and basic buffer solutions. In vitro release experiments were conducted using Franz diffusion system to monitor the controlled delivery fashion of gels matrices. Results concluded that depot gels exhibit controlled delivery fashion with maximum release at pH 7.4 and 37 ± 2 °C. The biocompatible nature of blank gels samples was assessed by MTT assay against Vero cell lines and was found safe. While killing ability of 5-FU encapsulated gels was evaluated against HeLa (19 ± 0.22 µg/ml; 23 ± 0.55 µg/ml) and MCF-7 (21 ± 0.06 µg/ml and 22 ± 0.34 µg/ml) cancer cell lines and were found effective to kill cancer cells. Histopathological study showed that gels depot is safe with no harmful effects on major organs. The in vivo bioavailability in rabbits showed controlled release (Cmax, 4465.78 ± 1.99 ng/ml) in comparison to free drug (Cmax, 4883.73 ± 3.32 ng/ml) administration after subcutaneous injection.


Alginates , Fluorouracil , Alginates/chemistry , Animals , Biological Availability , Delayed-Action Preparations/pharmacology , Fluorouracil/chemistry , Fluorouracil/pharmacology , Gels/chemistry , Humans , Hydrogels/chemistry , Rabbits , Rheology
18.
PLoS One ; 17(3): e0266296, 2022.
Article En | MEDLINE | ID: mdl-35358270

The major goal of this project was to formulate iodine-based self nano-emulsifying drug delivery system to provide improve antimicrobial activity and enhanced mucosal residence time via mucus penetration. Iodine SNEDDS (Self nano-emulsifying drug delivery system) with different concentration were formulated using castor oil as the oil phase, cremophor ethoxylated (CrEL) as a surfactant and after screening a number of vehicles, PEG 400 was employed as co-surfactant. Self-emulsification time, thermodynamic stability tests, robustness to dilution, percent transmittance, droplet size, and drug release were measured. Ternary phase diagrams were plotted to determine the area of emulsification. When compared to the commercial formulation, dissolving experiments revealed that the iodine from the SNEDDS enhanced aqueous solubility. In-vitro iodine release was determined to be around 15% per hour, with muco-adhesive and, muco-penetrating characteristics showing a 38-fold improvement. Furthermore, SNEDDS demonstrated significant antibacterial efficacy against Escherichia coli and Staphylococcus aureus. Similarly, when compared to marketed drugs, in-vitro drug absorption profile from the manufactured SNEDDS shown to be much higher. According to these results iodine containing SNEDDS could be a useful new formulation for iodine mucosal usage.


Iodine , Nanoparticles , Administration, Oral , Biological Availability , Delivery, Obstetric , Drug Delivery Systems/methods , Emulsions , Excipients , Female , Humans , Mucus , Particle Size , Pregnancy , Solubility , Surface-Active Agents
19.
Gels ; 8(3)2022 Mar 21.
Article En | MEDLINE | ID: mdl-35323309

In this study, we report the highly responsive chitosan-based chemically cross-linked nanomatrices, a nano-version of hydrogels developed through modified polymerization reaction for solubility improvement of poorly soluble drug simvastatin. The developed nanomatrices were characterized for solubilization efficiency, swelling studies, sol-gel analysis, in vitro drug release studies, DSC, FTIR, XRD, SEM, particle size analysis, and stability studies. An in vivo acute toxicity study was conducted on female Winstor rats, the result of which endorsed the safety and biocompatibility of the system. A porous and fluffy structure was observed under SEM analysis, which supports the great swelling tendency of the system that further governs the in vitro drug release. Zeta sizer analyzed the particle size in the range of 227.8 ± 17.8 nm. Nano sizing and grafting of hydrophilic excipients to the nanomatrices system explains this shift of trend towards the enhancement of solubilization efficiency, and, furthermore, the XRD results confirmed the amorphous nature of the system. FTIR and DSC analysis confirmed the successful grafting and stability to the system. The developed nanomatrices enhanced the release characteristics and solubility of simvastatin significantly and could be an effective technique for solubility and bioavailability enhancement of other BCS class-II drugs. Due to enhanced solubility, efficient method of preparation, excellent physico-chemical features, and rapid and high dissolution and bio-compatibility, the developed nanomatrices may be a promising approach for oral delivery of hydrophobic drugs.

20.
Curr Drug Deliv ; 19(10): 1102-1115, 2022.
Article En | MEDLINE | ID: mdl-35301948

BACKGROUND: Chronic wound healing is a major challenge for the health care system around the globe. The current study was conducted to develop and characterize chemically cross-linked polyethylene glycol-co-poly (AMPS) hydrogel membranes to enhance the wound healing efficiency of antibiotic mupirocin (MP). METHODS: Free radical polymerization technique was used to develop hydrogel membranes. In an aqueous medium, polymer PEG-4000 was cross-linked with the monomer 2-acrylamido-2-methylpropane sulfonic acid (AMPS) in the presence of initiators ammonium peroxide sulfate (APS) and sodium hydrogen sulfite (SHS). N, N-Methylene-bis-acrylamide (MBA) was used as a cross-linker in preparing hydrogel membranes. Developed membranes were spherical, transparent, and had elasticity. FTIR, TGA/DSC, and SEM were used to characterize the polymeric system. Swelling behavior, drug loading, and release pattern at pH of 5.5 and 7.4, irritation study, ex vivo drug permeation, and deposition study were also evaluated. RESULTS: Formed membranes were spherical, transparent, and had elasticity. The formation of a stable polymeric network was confirmed by structural and thermal analysis. Evaluation of the drug permeability in the skin showed good permeation and retention capabilities. No irritancy to the skin was observed. CONCLUSION: Based on the results obtained, the present study concluded that the formulated stable network might be an ideal network for the delivery of mupirocin in skin infections.


Hydrogels , Mupirocin , Delayed-Action Preparations/chemistry , Hydrogels/chemistry , Polyethylene Glycols , Polymers/chemistry , Wound Healing
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