PMID- 31758056
OWN - NLM
STAT- MEDLINE
DCOM- 20201103
LR  - 20210110
IS  - 2045-2322 (Electronic)
IS  - 2045-2322 (Linking)
VI  - 9
IP  - 1
DP  - 2019 Nov 22
TI  - Fabrication of Second Generation Smarter PLGA Based Nanocrystal Carriers for 
      Improvement of Drug Delivery and Therapeutic Efficacy of Gliclazide in Type-2 
      Diabetes Rat Model.
PG  - 17331
LID - 10.1038/s41598-019-53996-4 [doi]
LID - 17331
AB  - Drug delivery and therapeutic challenges of gliclazide, a BCS class II drug used 
      in type 2 diabetes mellitus (T2DM) can be overcome by exploring smarter carriers 
      of second-generation nanocrystals (SGNCs). A combined method of emulsion 
      diffusion, high-pressure homogenization and solvent evaporation method were 
      employed in the preparation of gliclazide loaded poly (D, L-lactide-co-glycolide) 
      (PLGA) SGNCs. Taguchi experimental design was adopted in fabrication of 
      Gliclazide SGNc using Gliclazide -PLGA ratio at 1:0.5, 1:0.75, 1:1 with 
      stabilizer (Poloxamer-188, PEG 4000, HPMC E15 at 0.5, 0.75, 1% w/v). The 
      formulated gliclazide of SGNCs were investigated for physicochemical properties, 
      in vitro drug release, and in vivo performance studies using type-2 diabetes rat 
      model. The formulation (SGNCF1) with Drug: PLGA 1: 0.5 ratio with 0.5% w/v 
      Poloxamer-188 produced optimized gliclazide SGNCs. SGNCF1 showed spherical shape, 
      small particle size (106.3 +/- 2.69 nm), good zeta potential (-18.2 +/- 1.30 mV), 
      small PDI (0.222 +/- 0.104) and high entrapment efficiency (86.27 +/- 0.222%). The 
      solubility, dissolution rate and bioavailability of gliclazide SGNCs were 
      significantly improved compared to pure gliclazide. The findings emphasize 
      gliclazide SGNCs produce faster release initially, followed by delayed release 
      with improved bioavailability, facilitate efficient delivery of gliclazide in 
      T2DM with better therapeutic effect.
FAU - Panda, Bibhu Prasad
AU  - Panda BP
AUID- ORCID: 0000-0002-7392-4883
AD  - Department of Pharmaceutical Technology, School of Pharmacy, Taylor's University, 
      Lakeside Campus, No 1, Jalan Taylor's, 47500, Subang Jaya, Selangor, Malaysia. 
      bibhuprasad25@yahoo.co.in.
FAU - Krishnamoorthy, Rachna
AU  - Krishnamoorthy R
AD  - Department of Pharmaceutical Technology, School of Pharmacy, Taylor's University, 
      Lakeside Campus, No 1, Jalan Taylor's, 47500, Subang Jaya, Selangor, Malaysia.
FAU - Bhattamisra, Subrat Kumar
AU  - Bhattamisra SK
AD  - Department of Life Sciences, School of Pharmacy, International Medical 
      University, Kuala Lumpur, 57000, Malaysia. bhattamisra@yahoo.co.in.
FAU - Shivashekaregowda, Naveen Kumar Hawala
AU  - Shivashekaregowda NKH
AUID- ORCID: 0000-0001-7417-5004
AD  - School of Pharmacy, Taylor's University, Lakeside Campus, No 1, Jalan Taylor's, 
      47500, Subang Jaya, Selangor, Malaysia.
FAU - Seng, Low Bin
AU  - Seng LB
AD  - School of Medicine, Taylor's University, Lakeside Campus, No 1, Jalan Taylor's, 
      47500, Subang Jaya, Selangor, Malaysia.
FAU - Patnaik, Sujata
AU  - Patnaik S
AD  - University College of Pharmaceutical Sciences, Kakatiya University, Warangal, 
      Telangana, India.
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20191122
PL  - England
TA  - Sci Rep
JT  - Scientific reports
JID - 101563288
RN  - 0 (Delayed-Action Preparations)
RN  - 0 (Hypoglycemic Agents)
RN  - 1SIA8062RS (Polylactic Acid-Polyglycolic Acid Copolymer)
RN  - 25X51I8RD4 (Niacinamide)
RN  - 5W494URQ81 (Streptozocin)
RN  - G4PX8C4HKV (Gliclazide)
SB  - IM
MH  - Animals
MH  - Biological Availability
MH  - Delayed-Action Preparations
MH  - Diabetes Mellitus, Experimental/*drug therapy
MH  - Diabetes Mellitus, Type 2/*drug therapy
MH  - Disease Models, Animal
MH  - Gliclazide/*administration & dosage/chemistry/pharmacokinetics
MH  - Hypoglycemic Agents/*administration & dosage/chemistry/pharmacokinetics
MH  - Male
MH  - Nanoparticles/chemistry
MH  - Niacinamide/adverse effects
MH  - Particle Size
MH  - Polylactic Acid-Polyglycolic Acid Copolymer/*chemistry
MH  - Rats
MH  - Streptozocin/adverse effects
PMC - PMC6874704
COIS- The authors declare no competing interests.
EDAT- 2019/11/24 06:00
MHDA- 2020/11/04 06:00
PMCR- 2019/11/22
CRDT- 2019/11/24 06:00
PHST- 2019/05/16 00:00 [received]
PHST- 2019/11/05 00:00 [accepted]
PHST- 2019/11/24 06:00 [entrez]
PHST- 2019/11/24 06:00 [pubmed]
PHST- 2020/11/04 06:00 [medline]
PHST- 2019/11/22 00:00 [pmc-release]
AID - 10.1038/s41598-019-53996-4 [pii]
AID - 53996 [pii]
AID - 10.1038/s41598-019-53996-4 [doi]
PST - epublish
SO  - Sci Rep. 2019 Nov 22;9(1):17331. doi: 10.1038/s41598-019-53996-4.