Surfactant and Polymer‐Based Self‐Assemblies for Encapsulation, Protection, and Release of Nutraceuticals

Afzal, Saima; Lone, Mohd Sajid; Kaur, Pawandeep; Ahanger, Firdous Ahmad; Nazir, Nighat; Dar, Aijaz Ahmad

doi:10.1002/9781119746843.ch16

Cited by 1 publication

(1 citation statement)

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“…Different types of lipid-based systems consisting of simple oil solution to complex mixtures of oil, surfactants, co-surfactants and polymers have been developed in recent years. Lipid-based systems can be tailored by changing the composition and concentration of excipients to make them suitable for wide variety of drugs and can be applied to different dosage forms to various routes of administration [7].…”

Section: Introductionmentioning

confidence: 99%

Formulation development, optimization and characterization of Pemigatinib-loaded supersaturable self-nanoemulsifying drug delivery systems

Reddy

Gubbiyappa

2022

Futur J Pharm Sci

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Background Pemigatinib is a small molecule tyrosine kinase inhibitor of fibroblast growth factor receptor inhibitors. The oral bioavailability of Pemigatinib is constricted due to its limited solubility at physiological pH. It is essential to develop a novel formulation of Pemigatinib to improve the intrinsic solubility and to reduce the pharmacokinetic variability. Self-nanoemulsifying drug delivery system is an effective, smart and more adequate formulation approach for poorly soluble drugs. Different from conventional self-nanoemulsifying drug delivery system, a supersaturable self-nanoemulsifying drug delivery system of Pemigatinib was prepared by using a supersaturation promoter. Results Among all the oils, Captex® 300 have shown maximum solubility of Pemigatinib. Considering the solubilization potential and emulsification ability Kolliphor®RH 40 was selected as surfactant. Transcutol®HP was selected as co-surfactant. The composition of oil, surfactant and co-surfactant was identified using phase diagrams and further adjusted by simplex-lattice design. HPMC K4M as precipitation inhibitor at 5% concentration resulted in effective supersaturating with increased self-emulsification time. The droplet of sSNEDDS ranges from 166.78 ± 3.14 to 178.86 ± 1.24 nm with PDI 0.212 – 0.256, which is significantly smaller than that observed with plain SNEDDS. TEM images revealed the spherical shape of the nanodroplets. The final optimized formulation formed spontaneous nanoemulsion within 15 secs when added to physiological fluids. The percent transmittance of the diluted formulation was found to be 99.12 ± 0.46. The viscosity was found to be 574 ± 26 centipoises indicating the good flow ability. FTIR and DSC studies indicated the amorphization of the drug. The dissolution profile of sSNEDDS indicated the faster release of drug compared to both pure drug suspension and SNEDDS formulation. The drug release rate is directly proportional to the concentration of the drug. The drug release from the insoluble matrix is a square root of time-dependent Fickian diffusion process. The formulation was found to be stable and transparent at all pH values and the percent transmittance was more than 95%. Any kind of separation or precipitation was not observed at different temperatures cycles. No significant difference was observed with all the samples exposed at different storage conditions. Conclusions This study demonstrated the feasibility of stabilizing and improving the in-vitro performance of self-nanoemulsifying drug delivery systems of Pemigatinib by incorporating HPMC K4M as precipitation inhibitor.

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Section: Introductionmentioning

confidence: 99%