Temperature-dependent solubility
data of bioactive compound hesperidin
has not been reported in any solvent in the literature so far. Therefore,
the aim of the current study was to measure the solubility of bioactive
compound hesperidin in six different pure solvents namely water, ethanol,
isopropyl alcohol (IPA), propylene glycol (PG), poly(ethylene glycol)-400
(PEG-400), and 1-butanol from (298.15 to 333.15) K using the shake
flask method. The experimental solubilities of hesperidin were regressed
by Apelblat equation with root-mean-square deviations in the range
of 6.32·10–7 to 0.184 in all solvents investigated.
The correlation coefficients in pure solvents were observed in the
range of 0.995 to 0.999. The mole fraction solubility of hesperidin
was found to be higher in PEG-400 (6.33·10–3 at 298.15 K) and PG (5.35·10–4 at 298.15
K) as compared to water (1.47·10–7 at 298.15
K), ethanol (3.45·10–5 at 298.15 K), IPA (1.53·10–5 at 298.15 K), and 1-butanol (3.15·10–4 at 298.15 K). The data of the current study could be useful in crystallization/purification
and formulation development of hesperidin in the chemical/pharmaceutical
industry.
Objective: Insulin is a hormone used in the treatment of diabetes mellitus. Multiple injections of insulin every day may causes pain, allergic reactions at injection site, which lead to low patient compliance. The aim of this work was to develop and evaluate an efficient solid lipid nanoparticle (SLN) carrier for oral delivery of insulin. Methods: SLNs were prepared by double emulsion solvent evaporation (w/o/w) technique, employing glyceryltrimyristate (Dynasan 114) as lipid phase and soy lecithin and polyvinyl alcohol as primary and secondary emulsifier, respectively, and evaluated in vitro for particle size, polydispersity index (PDI) and drug entrapment. Results: Among the eight different developed formulae (F1-F8), F7 showed an average particle size (99 nm), PDI (0.021), high entrapment of drug (56.5%). The optimized formulation (F7) was further evaluated by FT-IR, DSC, XRD, in vitro release, permeation, stability, bioavailability and pharmacological studies. Insulin-loaded SLNs showed better protection from gastrointestinal environment as evident from the relative bioavailability, which was enhanced five times as compared to the insulin solution. A significant enhancement of relative bioavailability of insulin was observed, i.e. approximately five times of pure insulin solution when loaded in SLN (8.26% versus 1.7% only).
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