Evidence map›Paper›PMID 30453628›Full record

ArticlePharmaceutics2018

Synthesis and Characterization of a Biomimetic Formulation of Clofazimine Hydrochloride Microcrystals for Parenteral Administration.

Mikhail D Murashov, Jennifer Diaz-Espinosa, Vernon LaLone, Joel W Y Tan, Raluca Laza, Xueding Wang, Kathleen A Stringer, Gus R Rosania

Open access · goldAbstract read
In one paragraph

Article in Pharmaceutics, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.

0numbers the graph read from it
0cells of the map it votes in
11citing papers in PubMed
2.3field-weighted citation impact, top 13% of its field
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

11 citing papers in PubMed, 18 citations in OpenAlex.

  1. Article
  2. Review
  3. Article
  4. Clofazimine for the treatment of tuberculosis.Frontiers in pharmacology · 2023
    Review
  5. Review
  6. Novel Administration of Clofazimine for the Treatment ofOpen forum infectious diseases · 2020
    Article
  7. Article
  8. Article
  9. Leprosy stigma & the relevance of emergent therapeutic options.The Indian journal of medical research · 2020
    Article
  10. Review
  11. Article
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

8 authors at 1 institution in 1 country.

Mikhail D MurashovDepartment of Pharmaceutical Sciences, University of Michigan, Ann Arbor, MI 48109, USA. murashov@umich.edu.ORCID 0000-0001-6300-6109
Jennifer Diaz-EspinosaDepartment of Pharmaceutical Sciences, University of Michigan, Ann Arbor, MI 48109, USA. jendiaz@umich.edu.
Vernon LaLoneDepartment of Pharmaceutical Sciences, University of Michigan, Ann Arbor, MI 48109, USA. laloneve@umich.edu.ORCID 0000-0001-6043-8993
Joel W Y TanDepartment of Biomedical Engineering, University of Michigan, Ann Arbor, MI 48109, USA. tanjoel@umich.edu.
Raluca LazaDepartment of Pharmaceutical Sciences, University of Michigan, Ann Arbor, MI 48109, USA. rmlaza@umich.edu.
Xueding WangDepartment of Biomedical Engineering, University of Michigan, Ann Arbor, MI 48109, USA. xdwang@umich.edu.
Kathleen A StringerDepartment of Clinical Pharmacy, University of Michigan, Ann Arbor, MI, 48109, USA. stringek@umich.edu.ORCID 0000-0003-0238-7774
Gus R RosaniaDepartment of Pharmaceutical Sciences, University of Michigan, Ann Arbor, MI 48109, USA. grosania@umich.edu.ORCID 0000-0003-3214-5565
University of Michigan · US

Funding

Chemical Address Tags: A Cheminformatics & Image Data Management and Analysis Plan - SupplementR01GM078200 · NIGMS · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI ROSANIA, GUS R · 2006 to 2015
$4.2M
L-Carnitine As A Metabolic Biomarker of Drug Toxicity RiskR01GM127787 · NIGMS · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI ROSANIA, GUS R · 2019 to 2022
$2.0M
L-Carnitine Pharmacometabolomics in Sepsis (CaPS)R01GM111400 · NIGMS · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI STRINGER, KATHLEEN A · 2016 to 2019
$1.2M
MEDC Mi-TRAC award (Kickstart grant-216109) to GRR grant-216109National Institutes of Health P50 CA186786NIGMS NIH HHS R01 GM078200NIGMS NIH HHS R01 GM111400NIGMS NIH HHS R01 GM127787University of Michigan College of Pharmacy Upjohn AwardUniversity of Michigan MCubed
6 · The paper itself

Abstract

Clofazimine (CFZ) is a broad spectrum antimycobacterial agent recommended by the World Health Organization as a first line treatment for leprosy and second line treatment for multidrug resistant tuberculosis. Oral administration of CFZ leads to a red skin pigmentation side effect. Since CFZ is a weakly basic, red phenazine dye, the skin pigmentation side effect results from lipophilic partitioning of the circulating, free base (neutral) form of CFZ into the skin. Here, we developed a stable and biocompatible formulation of CFZ-HCl microcrystals that mimics the predominant form of the drug that bioaccumulates in macrophages, following long term oral CFZ administration. In mice, intravenous injection of these biomimetic CFZ-HCl microcrystals led to visible drug accumulation in macrophages of the reticuloendothelial system with minimal skin accumulation or pigmentation. In fact, no skin pigmentation was observed when the total amount of CFZ-HCl administered was equivalent to the total oral dose leading to maximal skin pigmentation. Thus, parenteral (injected or inhaled) biomimetic formulations of CFZ-HCl could be instrumental to avoid the pigmentation side effect of oral CFZ therapy.

Indexed as

adverse drug reaction (ADR)CFZ-induced skin pigmentationcrystal-like drug inclusion (CLDI)drug repurposingjet milling/micronizationmacrophagesmicronized crystals

Identifiers

PMID30453628
PMCPMC6321048
OpenAlexW2901925409

What OpenQuestion holds

Textmetadata
LicenceCC BY
Read underepoch 390

Registered trials

None linked

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.