Effect of PEGylation on drug uptake, biodistribution, and tissue toxicity of efavirenz–ritonavir loaded PAMAM G4 dendrimers

Kharwade, Rohini; Mahajan, Nilesh; More, Sachin; Warokar, Amol; Mendhi, Sachin; Dhobley, Akshay; Palve, Devendra

doi:10.1080/10837450.2023.2173230

Cited by 3 publications

(2 citation statements)

References 74 publications

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“…This mechanism showed an initial burst released during the 4 h when the concentration of the dissolved drug in the hydrogel vehicle was high. It was followed by a sustained release for the duration up to 24 h. This happened because Tz was entrapped in TFs and the fraction of the Tz particles were dispersed in the homogeneous hydrogel matrix [ 31 , 32 ]. The Korsmeyer–Peppas release exponent data showed a non-Fickian anomalous release with an n value of 0.533.…”

Section: Discussionmentioning

confidence: 99%

DOE-Assisted Formulation, Optimization, and Characterization of Tioconazole-Loaded Transferosomal Hydrogel for the Effective Treatment of Atopic Dermatitis: In Vitro and In Vivo Evaluation

Kharwade

Ali

Gangane

et al. 2023

Gels

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The present study was performed to determine the therapeutic effects of tioconazole (Tz)-loaded novel transferosome carriers (TFs) for the treatment of atopic dermatitis (AD). Method: Tioconazole transferosomes suspension (TTFs) was formulated and optimized using a 32 factorial design. After that, the optimized batch of TTFs loaded into Carbopol 934 and sodium CMC was prepared with hydrogel and noted as TTFsH. Subsequently, it was evaluated for pH, spread ability, drug content, in vitro drug release, viscosity, in vivo scratching and erythema score, skin irritation, and histopathology study. Result: The optimized batch of TTFs (B4) showed the values of vesicle size, flux, and entrapment efficiency to be 171.40 ± 9.03 nm, 48.23 ± 0.42, and 93.89 ± 2.41, respectively. All batches of TTFsH showed sustained drug release for up to 24 h. The F2 optimized batch released Tz in an amount of 94.23 ± 0.98% with a flux of 47.23 ± 0.823 and followed the Higuchi kinetic model. The in vivo studies provided evidence that the F2 batch of TTFsH was able to treat atopic dermatitis (AD) by reducing the erythema and the scratching score compared to that of the marketed formulation (Candiderm cream, Glenmark). The histopathology study supported the result of the erythema and scratching score study with intact skin structure. It showed that a formulated low dose of TTFsH was safe and biocompatible to both the dermis and the epidermis layer of skin. Conclusion: Thus, a low dose of F2-TTFsH is a promising tool that effectively targeted the skin for the topical delivery of Tz to treat atopic dermatitis symptoms.

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Section: Discussionmentioning

confidence: 99%

DOE-Assisted Formulation, Optimization, and Characterization of Tioconazole-Loaded Transferosomal Hydrogel for the Effective Treatment of Atopic Dermatitis: In Vitro and In Vivo Evaluation

Kharwade

Ali

Gangane

et al. 2023

Gels

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“…To prevent the growth of smaller dendritic impurities, meticulous measures must be taken to ensure that the activating agent itself cannot initiate new growth. Poly (amidoamines) (PAMAM) and poly (propylene imine) dendrimers seem particularly noteworthy among the many divergent syntheses studied to date [ 22 , 23 ].…”

Section: Synthetic Strategiesmentioning

confidence: 99%

Phosphorus-carrying cascade molecules: inner architecture to biomedical applications

THIRUMALAI,

ELBOUGHDIRI,

HARINI

et al. 2023

Turkish Journal of Chemistry

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Cascade molecules are nearly uniform-sized macromolecules of small molecules or linear polymer cores built around symmetric branching units. A wide range of biological properties can be achieved with phosphorus-containing dendrimers, depending on their terminal functions, ranging from biomaterials to imaging, drug delivery, and acting as a drug by themselves. This feature article presents significant examples of phosphorus-containing dendrimers used to develop biochips, support cell cultures, carry or deliver biomacromolecules and drugs, bioimaging, and combinational benefits. Because of the thermal stability, ferrocene function, and physical and chemical properties of phosphorus, dendrimers show greater rigidity, mobility, and strength. These dendrimers will be discussed as having a favorable effect on cell growths, especially on neuronal cells, as well as human immune cells like natural killer cells and monocytes, which have a crucial part in preventing cancerous and viral infections. Several phosphorus dendrimers are effective as drugs by themselves (drug per se) and show their activity against neurodegenerative diseases, cancer, inflammation, ocular hypertension, and transmissible spongiform encephalopathies (TSEs) in both in vivo and in vitro. The present review discusses the synthetic route, fabrications, and biomedical applications of phosphorus-containing dendrimers. The toxicity of these dendrimers was also reported.

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Synthetic Polymers as Antibacterial and Antiviral Agents

Mousavi,

Hashemi,

Yari Kalashgrani

et al. 2024

ACS Symposium Series

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Effect of PEGylation on drug uptake, biodistribution, and tissue toxicity of efavirenz–ritonavir loaded PAMAM G4 dendrimers

Cited by 3 publications

References 74 publications

DOE-Assisted Formulation, Optimization, and Characterization of Tioconazole-Loaded Transferosomal Hydrogel for the Effective Treatment of Atopic Dermatitis: In Vitro and In Vivo Evaluation

DOE-Assisted Formulation, Optimization, and Characterization of Tioconazole-Loaded Transferosomal Hydrogel for the Effective Treatment of Atopic Dermatitis: In Vitro and In Vivo Evaluation

Phosphorus-carrying cascade molecules: inner architecture to biomedical applications

Synthetic Polymers as Antibacterial and Antiviral Agents

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