PMID- 32961738
OWN - NLM
STAT- PubMed-not-MEDLINE
LR  - 20201023
IS  - 1999-4923 (Print)
IS  - 1999-4923 (Electronic)
IS  - 1999-4923 (Linking)
VI  - 12
IP  - 9
DP  - 2020 Sep 19
TI  - Selection of Cryoprotectant in Lyophilization of Progesterone-Loaded Stearic Acid 
      Solid Lipid Nanoparticles.
LID - 10.3390/pharmaceutics12090892 [doi]
LID - 892
AB  - Cryoprotectants are often required in lyophilization to reduce or eliminate 
      agglomeration of solute or suspended materials. The aim of this study was to 
      select a cryoprotecting agent and optimize its concentration in a solid lipid 
      nanoparticle formulation. Progesterone-loaded stearic acid solid lipid 
      nanoparticles (SA-P SLNs) were prepared by hot homogenization with high speed 
      mixing and sonication. The stearic acid content was 4.6% w/w and progesterone was 
      0.46% w/w of the initial formulation. Multiple surfactants were evaluated, and a 
      lecithin and sodium taurocholate system was chosen. Three concentrations of 
      surfactant were then evaluated, and a concentration of 2% w/w was chosen based on 
      particle size, polydispersity, and zeta potential. Agglomeration of SA-P SLNs 
      after lyophilization was observed as measured by increased particle size. 
      Dextran, glycine, mannitol, polyvinylpyrrolidone (PVP), sorbitol, and trehalose 
      were evaluated as cryoprotectants by both an initial freeze-thaw analysis and 
      after lyophilization. Once selected as the cryoprotectant, trehalose was 
      evaluated at 5%, 10%, 15%, and 20% for optimal concentration, with 20% trehalose 
      being finally selected as the level of choice. Evaluation by DSC confirmed 
      intimate interaction between stearic acid and progesterone in the SA-P SLNs, and 
      polarized light microscopy shows successful lyophilization of the trehalose/SA-P 
      SLN. A short term 28-day stability study suggests the need for refrigeration of 
      the final lyophilized SA-P SLNs in moisture vapor impermeable packaging.
FAU - Amis, Timothy M
AU  - Amis TM
AD  - Department of Basic Pharmaceutical Sciences, Fred Wilson School of Pharmacy, High 
      Point University, High Point, NC 27268, USA.
FAU - Renukuntla, Jwala
AU  - Renukuntla J
AD  - Department of Basic Pharmaceutical Sciences, Fred Wilson School of Pharmacy, High 
      Point University, High Point, NC 27268, USA.
FAU - Bolla, Pradeep Kumar
AU  - Bolla PK
AUID- ORCID: 0000-0001-5049-3550
AD  - Department of Basic Pharmaceutical Sciences, Fred Wilson School of Pharmacy, High 
      Point University, High Point, NC 27268, USA.
FAU - Clark, Bradley A
AU  - Clark BA
AD  - Department of Basic Pharmaceutical Sciences, Fred Wilson School of Pharmacy, High 
      Point University, High Point, NC 27268, USA.
LA  - eng
PT  - Journal Article
DEP - 20200919
PL  - Switzerland
TA  - Pharmaceutics
JT  - Pharmaceutics
JID - 101534003
PMC - PMC7560102
OTO - NOTNLM
OT  - cryoprotectant
OT  - freezing rate
OT  - lyophilization
OT  - solid lipid nanoparticles
OT  - surfactants
OT  - trehalose
COIS- The authors declare no conflict of interest.
EDAT- 2020/09/24 06:00
MHDA- 2020/09/24 06:01
PMCR- 2020/09/01
CRDT- 2020/09/23 01:01
PHST- 2020/08/18 00:00 [received]
PHST- 2020/09/10 00:00 [revised]
PHST- 2020/09/16 00:00 [accepted]
PHST- 2020/09/23 01:01 [entrez]
PHST- 2020/09/24 06:00 [pubmed]
PHST- 2020/09/24 06:01 [medline]
PHST- 2020/09/01 00:00 [pmc-release]
AID - pharmaceutics12090892 [pii]
AID - pharmaceutics-12-00892 [pii]
AID - 10.3390/pharmaceutics12090892 [doi]
PST - epublish
SO  - Pharmaceutics. 2020 Sep 19;12(9):892. doi: 10.3390/pharmaceutics12090892.