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Buparvaquone Nanostructured Lipid Carrier: Development of an Affordable Delivery System for the Treatment of Leishmaniases.

Abstract Buparvaquone (BPQ), a veterinary drug, was formulated as nanostructured lipid carriers (NLC) for leishmaniases treatment. The formulation design addressed poor water solubility of BPQ and lack of human drug delivery system. The DSC/TG and microscopy methods were used for solid lipids screening. Softisan® 154 showed highest BPQ solubility in both methods. The BPQ solubility in liquid lipids using HPLC revealed Miglyol® 812 as the best option. Response surface methodology (RSM) was used to identify the optimal Softisan154 : Miglyol 812 ratios (7 : 10 to 2 : 1) and Kolliphor® P188 and Tween® 80 concentration (>3.0% w/w) aiming for z-average in the range of 100-300 nm for macrophage delivery. The NLC obtained by high-pressure homogenization showed low z-averages (<350 nm), polydispersity (<0.3), and encapsulation efficiency close to 100%. DSC/TG and microscopy in combination proved to be a powerful tool to select the solid lipid. The relationship among the variables, demonstrated by a linear mathematical model using RSM, allowed generating a design space. This design space showed the limits in which changes in the variables influenced the z-average. Therefore, these drug delivery systems have the potential to improve the availability of affordable medicines due to the low cost of raw materials, using well established, reliable, and feasible scale-up technology.
PMID
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Authors

Mayor MeshTerms

Drug Delivery Systems

Keywords
Journal Title biomed research international
Publication Year Start




PMID- 28255558
OWN - NLM
STAT- MEDLINE
DA  - 20170303
DCOM- 20170313
LR  - 20170313
IS  - 2314-6141 (Electronic)
VI  - 2017
DP  - 2017
TI  - Buparvaquone Nanostructured Lipid Carrier: Development of an Affordable Delivery 
      System for the Treatment of Leishmaniases.
PG  - 9781603
LID - 10.1155/2017/9781603 [doi]
AB  - Buparvaquone (BPQ), a veterinary drug, was formulated as nanostructured lipid
      carriers (NLC) for leishmaniases treatment. The formulation design addressed poor
      water solubility of BPQ and lack of human drug delivery system. The DSC/TG and
      microscopy methods were used for solid lipids screening. Softisan(R) 154 showed
      highest BPQ solubility in both methods. The BPQ solubility in liquid lipids using
      HPLC revealed Miglyol(R) 812 as the best option. Response surface methodology
      (RSM) was used to identify the optimal Softisan154 : Miglyol 812 ratios (7 : 10
      to 2 : 1) and Kolliphor(R) P188 and Tween(R) 80 concentration (&gt;3.0% w/w) aiming 
      for z-average in the range of 100-300 nm for macrophage delivery. The NLC
      obtained by high-pressure homogenization showed low z-averages (&lt;350 nm),
      polydispersity (&lt;0.3), and encapsulation efficiency close to 100%. DSC/TG and
      microscopy in combination proved to be a powerful tool to select the solid lipid.
      The relationship among the variables, demonstrated by a linear mathematical model
      using RSM, allowed generating a design space. This design space showed the limits
      in which changes in the variables influenced the z-average. Therefore, these drug
      delivery systems have the potential to improve the availability of affordable
      medicines due to the low cost of raw materials, using well established, reliable,
      and feasible scale-up technology.
FAU - Monteiro, Lis Marie
AU  - Monteiro LM
AUID- ORCID: 0000-0001-6409-0672
AD  - Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of Sao
      Paulo, Professor Lineu Prestes Av 580, Cidade Universitaria, 05508-000 Sao Paulo,
      SP, Brazil.
FAU - Lobenberg, Raimar
AU  - Lobenberg R
AD  - Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, 8613
      114th St NW, Edmonton, AB, Canada T6G 2H7.
FAU - Cotrim, Paulo Cesar
AU  - Cotrim PC
AD  - Seroepidemiology, Cellular and Molecular Immunology Laboratory, Institute of
      Tropical Medicine, University of Sao Paulo, Dr. Eneas de Carvalho Aguiar 470,
      Jardim America, 05403-000 Sao Paulo, SP, Brazil.
FAU - Barros de Araujo, Gabriel Lima
AU  - Barros de Araujo GL
AUID- ORCID: 0000-0001-7590-3587
AD  - Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of Sao
      Paulo, Professor Lineu Prestes Av 580, Cidade Universitaria, 05508-000 Sao Paulo,
      SP, Brazil.
FAU - Bou-Chacra, Nadia
AU  - Bou-Chacra N
AUID- ORCID: 0000-0002-5271-5468
AD  - Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of Sao
      Paulo, Professor Lineu Prestes Av 580, Cidade Universitaria, 05508-000 Sao Paulo,
      SP, Brazil.
LA  - eng
PT  - Journal Article
DEP - 20170201
PL  - United States
TA  - Biomed Res Int
JT  - BioMed research international
JID - 101600173
RN  - 0 (Drug Carriers)
RN  - 0 (Lipids)
RN  - 0 (Naphthoquinones)
RN  - 0354RT7LG4 (buparvaquone)
SB  - IM
MH  - Analysis of Variance
MH  - Calorimetry, Differential Scanning
MH  - Chemistry, Pharmaceutical
MH  - Crystallization
MH  - Drug Carriers/*chemistry
MH  - *Drug Delivery Systems
MH  - Humans
MH  - Leishmaniasis/*drug therapy
MH  - Lipids/*chemistry
MH  - Microscopy
MH  - Nanostructures/*chemistry
MH  - Naphthoquinones/pharmacology/*therapeutic use
MH  - Solubility
MH  - Static Electricity
PMC - PMC5309432
COI - The authors declare that there is no conflict of interests regarding the
      publishing of this paper.
EDAT- 2017/03/04 06:00
MHDA- 2017/03/14 06:00
CRDT- 2017/03/04 06:00
PHST- 2016/09/08 [received]
PHST- 2017/01/05 [accepted]
AID - 10.1155/2017/9781603 [doi]
PST - ppublish
SO  - Biomed Res Int. 2017;2017:9781603. doi: 10.1155/2017/9781603. Epub 2017 Feb 1.

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