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Objective of the research was to potentiate solubility of Rosuvastatin by nanogels synthesized by free radical polymerization. Surface morphology and structural compatibility were studied through scanning electron microscopy (SEM) and Fourier Transform Infrared (FTIR) spectroscopy. Zeta sizer was used for particle size analysis. Swelling, in-vitro release and solubility studies were accomplished in different media. Similarly, results of in-vitro release of nanogels and commercially available tablets of Rosuvastatin were compared in different dissolution media. Biocompatibility study was performed in healthy rabbits for safety profile. FTIR spectroscopy confirmed the presence of corresponding peaks of respective functional groups of individual constituents and that of the drug in unloaded and loaded nanogels. SEM images depicted the fluffy appearance of nanogels with small pores inside the structure. Particle size of the optimized formulation was in the range of 217.70 ± 2.23 for unloaded and 257.33 ± 2.11 for loaded nanogels. Percent drug loading, in-vitro drug release and solubility profiles were also satisfactory. In comparison with commercially available tablet Rovista®, in-vitro release profiles of synthesized nanogels showed better response. Moreover, synthesized nanogels were also biocompatible. It was concluded that the solubility of Rosuvastatin was potentially enhanced by nanogels and such formulation can also be used for other poorly soluble drugs. [ABSTRACT FROM AUTHOR]

Purpose of the current study was to improve the oral effectiveness of 5-fluorouracil (5-FU) by developing novel controlled, combinatorial drug delivery system (nCDDS) for co-delivery of 5-FU and leucovorin calcium (LC) for colon targeting. On the basis of results obtained, novel controlled, combinatorial drug delivery system could be an effective strategy for the colon targeting of 5-FU and LC. Free radical polymerization method was tuned and used to fabricate this nCDDS. The nCDDS is synthesized in two steps, first synthesis of 5-FU/LC calcium loaded nanogels and second, pre-synthesized 5-FU and LC loaded nanogels were dispersed in pectin based polymerized matrix hard gel. The nanogels and nCDDS gels were characterized for network structure, thermal stability, and surface morphology. Swelling and in vitro release studies were carried out at different pH 1.2 and 7.4 both for naive nanogels and combined matrix gels. In vivo study of combinatorial gel was performed on rabbits by using HPLC method to estimate plasma drug concentration and pharmacokinetics parameters. Structure and thermal analysis confirmed the formation of stable polymeric network. SEM of nanogels and combinatorial gels showed that the spongy and rough edges particles and uniformly distributed in the combinatorial gel. The prepared nCDDS showed excellent water loving capacity and pH responsiveness. Combinatorial gel showed excellent characteristic for colonic delivery of drugs, which were confirmed by various in vitro and in vivo characterizations. Acute oral toxicity study of combinatorial gel confirmed the biocompatible and nontoxic characteristics of developed formulation. Conclusively, it can be found that nCDDS showed excellent properties regarding drug targeting in a controllable manner as compared to naive PEGylated nanogels. [ABSTRACT FROM AUTHOR]

Poor solubility is an ongoing issue and the graph of poorly soluble drugs has increased markedly which critically affect their dissolution, bioavailability, and clinical effects. This common issue needs to be addressed, for this purpose a series of polyethylene glycol (PEG-4000) based nanogels were developed by free radical polymerization technique to enhance the solubility, dissolution, and bioavailability of poorly soluble drug meloxicam (MLX), as improved solubility is the significant application of nanosystems. Developed nanogels formulations were characterized by FTIR, XRD, SEM, zeta sizer, percent equilibrium swelling, drug loaded content (DLC), drug entrapment efficiency (DEE), solubility studies, and in vitro dissolution studies. Furthermore, cytotoxicity studies were conducted in order to determine the bio-compatibility of the nanogels drug delivery system to biological environment. Nanogels particle size was found to be 156.19 ± 09.33 d.nm. Solubility study confirmed that the solubility of poorly soluble drug MLX was significantly enhanced up to 36 folds as compared to reference product (Mobic®). The toxicity study conducted on rabbits and MTT assay endorsed the safety of the developed nanogels formulations to the biological system. [ABSTRACT FROM AUTHOR]

The purpose of current research work was to synthesize and evaluate the cross‐linked ternary hydrogels using polyvinyl alcohol (PVA) and two monomers itaconic acid and methacrylic acid. Controlled combinatorial drug delivery systems (CCDDS) were synthesized by free radical solution polymerization method using ethylene glycol dimethacrylate (EGDMA) as cross‐linking agent. 5‐Fluorouracil (5‐FU) and leucovorin calcium (LC) were loaded in combination into synthesized gels for colonic delivery. Various characterizations such as Fourier transform infrared spectroscopy, differential scanning calorimetry, TGA, powder X‐ray diffraction, and scanning electron microscopy were performed to confirm the cross‐linking of functional groups, thermal stability, crystal structure, and surface morphology of developed formulations. Swelling and drug release was performed at higher and lower pH (1.2, 7.4) buffer solution. Increase in swelling was observed at higher pH 7.4. Cumulative percent release of 5‐FU and LC was 29.8% and 27.2% at pH 1.2, and 86.9% and 87.01% at pH 7.4, respectively. Kinetic modeling was applied on optimized hydrogel formulation, and the results showed that release of 5‐FU and LC best expressed by first‐order kinetic model with regression coefficient (R2) value 0.937 for 5‐FU and 0.963 for LC. Acute oral toxicity was performed on healthy rabbits, and results showed that the synthesized CCDDS is nontoxic and compatible with biological system. In vivo studies on rabbits were conducted using HPLC, and plasma drug concentration and pharmacokinetic parameters were estimated. Newly synthesized CCDDS showed a good pH‐responsive swelling and controlled drug delivery characteristics. CCDDS can be used as excellent carrier for various therapeutic agents, which are compatible with biological system. [ABSTRACT FROM AUTHOR]

The aim of this study was to formulate and evaluate acrylic acid‐based topical hydrogel patches of mupirocin for new pharmaceutical controlled release application. These cross‐linked hydrogel patches were synthesized by modified aqueous‐based polymerization technique. Acrylic acid was cross‐linked with 2‐acrylamido‐2‐methylpropanesulfonic acid (AMPS) with the help of cross‐linker N,N‐methylenebisacrylamide (MBA). Hydrogel patches were characterized by FTIR, TGA, DSC, SEM, swelling behavior, in vitro percent drug release at different pH, permeation across skin, ex vivo drug retention study, and irritation evaluation of mupirocin‐loaded hydrogels. Developed patches were spherical, thick, adhesive and with good elastic strength. FTIR confirmed the cross‐linking and formation of new structure having appropriate characteristics needed for controlled release delivery system. Dug (mupirocin) release through rabbit's skin was evaluated by Franz diffusion cell and up to 3,991.95 μg/L.5 cm2 was permeated, and drug retention in skin revealed substantial retention up to 1,261 μg/L.5 cm2. Formulated hydrogel patches were nonirritant to the skin up to 48 hr as validated by Draize patch test. Enhanced retention of drug in skin demonstrated good potential of topical delivery for skin bacterial infections. [ABSTRACT FROM AUTHOR]

Background: One of the major reasons for unsuccessful treatment outcomes among patients with drug-resistant tuberculosis (DR-TB) is the high rate of loss to follow-up (LTFU). However, in Pakistan, no qualitative study has been conducted to explore the perceptions of LTFU patients with regard to DR-TB treatment, the problems they face and the reasons for LTFU in detail., Methods: This was a qualitative study that involved semistructured, indepth, face-to-face interviews of 39 LTFU patients with DR-TB. All interviews were carried out in Pakistan's national language 'Urdu' using an interview guide in two phases: the first phase was from December 2020 to February 2021 among patients with extensively drug-resistant tuberculosis and the second phase from July 2021 to September 2021 among patients with multidrug-resistant tuberculosis., Results: The inductive thematic analysis of audio-recorded interviews generated the following four key themes, which were the major reasons reported by the participants of the current study to have led to LTFU: (1) patient-related factors, such as lack of awareness about the total duration of DR-TB treatment, fatigue from previous multiple failed episodes, lack of belief in treatment efficacy and perception of DR-TB as a non-curable disease; (2) medication-related factors, such as use of injectables, high pill burden, longer duration and adverse events; (3) socioeconomic factors, such as gender discrimination, poor socioeconomic conditions, non-supportive family members, social isolation and unemployment; and (4) service provider-related factors, such as distant treatment centres, non-availability of a qualified person, lack of adequate counselling and poor attitude of healthcare professionals., Conclusion: In the current study, patients' perceptions about DR-TB treatment, socioeconomic condition, medication and service provider-related factors emerged as barriers to the successful completion of DR-TB treatment. Increasing patients' awareness about the duration of DR-TB treatment, interacting sessions with successfully treated patients, availability of rapid drug susceptibility testing facilities at treatment centres, decentralising treatment and using the recently recommended all-oral regimen may further decrease the rate of LTFU., Competing Interests: Competing interests: None declared., (© Author(s) (or their employer(s)) 2024. Re-use permitted under CC BY-NC. No commercial re-use. See rights and permissions. Published by BMJ.)

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.

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., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)