Evidence map›Paper›PMID 35735686›Full record

ArticleGels (Basel, Switzerland)2022

Intranasal Delivery of Darunavir-Loaded Mucoadhesive In Situ Gel: Experimental Design, In Vitro Evaluation, and Pharmacokinetic Studies.

Anroop B Nair, Sunita Chaudhary, Hiral Shah, Shery Jacob, Vivek Mewada, Pottathil Shinu, Bandar Aldhubiab, Nagaraja Sreeharsha, Katharigatta N Venugopala, Mahesh Attimarad and 1 more

Abstract read
In one paragraph

Article in Gels (Basel, Switzerland), 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
24citing papers in PubMed, 1 pooled it
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

24 citing papers in PubMed, 1 synthesis or guideline pooled it.

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  14. Recent opportunities and application of gellan gum based drug delivery system for intranasal route.Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences · 2024
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4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

11 authors.

Anroop B NairDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi Arabia.ORCID 0000-0003-2850-8669
Sunita ChaudharyDepartment of Pharmaceutics, Arihant School of Pharmacy & BRI, Adalaj, Gandhinagar 382421, India.ORCID 0000-0001-6983-1134
Hiral ShahDepartment of Pharmaceutics, Arihant School of Pharmacy & BRI, Adalaj, Gandhinagar 382421, India.
Shery JacobDepartment of Pharmaceutical Sciences, College of Pharmacy, Gulf Medical University, Ajman 4184, United Arab Emirates.ORCID 0000-0003-1851-6673
Vivek MewadaDepartment of Pharmaceutics, Institute of Pharmacy, Nirma University, Ahmedabad 382481, India.
Pottathil ShinuDepartment of Biomedical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi Arabia.ORCID 0000-0003-4245-0803
Bandar AldhubiabDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi Arabia.ORCID 0000-0002-2684-4186
Nagaraja SreeharshaDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi Arabia.ORCID 0000-0002-2058-255X
Katharigatta N VenugopalaDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi Arabia.ORCID 0000-0003-0680-1549
Mahesh AttimaradDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi Arabia.ORCID 0000-0002-7007-9119
Jigar ShahDepartment of Pharmaceutics, Institute of Pharmacy, Nirma University, Ahmedabad 382481, India.ORCID 0000-0002-9375-528X

Funding

Deanship of Scientific Research, King Faisal University, Al Ahsa, Saudi Arabia AN000129
6 · The paper itself

Abstract

The clinical efficacy of antiretroviral therapy in NeuroAIDS is primarily limited by the low perfusion of the drug to the brain. The objective of the current investigation was to design and develop an in situ mucoadhesive gel loaded with darunavir to assess the feasibility of brain targeting through the intranasal route. Preliminary batches (F1−F9) were prepared and evaluated for various pharmaceutical characteristics. A full factorial design of the experiment was applied to optimize and assess the effect of two influencing variables (Carbopol 934P (X1) and Poloxamer 407 (X2)) on the response effects (gelation temperature (Y1) and % drug release (Y2) at 8 h). The data demonstrate that both influencing variables affect the response variables significantly (p < 0.05). The optimized formulation (F7) exhibited favorable rheological properties, adequate mucoadhesion, sustained drug release, and greater permeation across the nasal mucosa. An in vitro ciliotoxicity study confirms the nontoxicity of the optimized in situ gel (D7) on the nasal mucosa. An in vivo pharmacokinetic study in rats was performed to assess drug targeting to the brain following the nasal application of the selected in situ gel (D7). Significantly higher (p < 0.0001) Cmax (~4-fold) and AUC0-α (~3.5-fold) values were noticed in the brain after nasal application, as compared to the intravenous route. However, less systemic exposure to darunavir was noticed with nasal therapy, which confirms the low absorption of the drug into the central compartment. Overall, the data here demonstrate that the optimized in situ mucoadhesive nasal gel is effective in targeting darunavir to the brain by the nasal route and could be a viable option for the treatment of NeuroAIDS.

Indexed as

brain targetingdarunavirmucoadhesivenasal in situ gelNeuroAIDSoptimization

Identifiers

PMID35735686
PMCPMC9223067

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Registered trials

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.