An optimized PVP K30-poloxamer binary composition for SD carrier was developed. Tensile strength of SD can be considered as a response for experimental design to optimize SD.
Supramolecular mesoporous silica nanoparticles (MSNs) offer distinct properties as opposed to micron-sized silica particles in terms of their crystal structure, morphology–porosity, toxicity, biological effects, and others. MSN biocompatibility has touched the pharmaceutical realm to exploit its robust synthesis pathway for delivery of various therapeutic molecules including macromolecules and small-molecule drugs. This article provides a brief review of MSN history followed by special emphasis on the influencing factors affecting morphology–porosity characteristics. Its applications as the next-generation drug delivery system (NGDDS) particularly in a controlled release dosage form via an oral drug delivery system are also presented and shall be highlighted as oral delivery is the most convenient route of drug administration with the economical cost of development through to scale-up for clinical trials and market launch.
Background: Oral bioavailability of gliclazide, a hypoglycemic drug, is hindered by its low aqueous solubility. Improvement of solubility will enhance dissolution rate and in turn the bioavailability. This research aimed to formulate the solid dispersed gliclazide using a novel polyethylene glycol-polyvinyl caprolactam-polyvinyl acetate grafted copolymer (Soluplus®) as carrier to enhance in-vitro dissolution and to study drug-carrier physical interaction. Method: Final solid dispersion (SDGLC) containing drug:carrier (1:8 w/w) was prepared by solvent evaporation after drug-polymer miscibility study. The SDGLC powder was characterized by differential scanning calorimetry (DSC), attenuated total reflectance infra-red spectroscopy (ATR-IR), powder X-ray diffraction (PXRD), and scanning electron microscopy (SEM). SDGLC powder was filled in gelatin capsule after flowability and moisture analysis followed by assay, disintegration and in-vitro dissolution study. Results: Miscibility study showed negative values of free energy transfer indicating spontaneous solubilization of drug with increase in carrier concentration. Absence of sharp melting peak in SDGLC was observed by DSC. Reduced peak intensity at specific 2θ values in PXRD indicates loss of crystallinity in solid dispersion. Interaction to form H-bond between gliclazide and Soluplus® was evidenced by ATR-IR. SDGLC filled capsule resulted in 20% improved dissolution (approximately 20% higher) in 0.1(N) HCl and phosphate buffer pH 7.4 compared to physical mixture (gliclazide-Soluplus®) containing capsule. Conclusion: Soluplus® effectively enhanced gliclazide solubility in solid dispersed state and SDGLC powder filled capsules could provide pH independent and improved in-vitro dissolution for gliclazide.
Mesoporous silica (MPS), a carrier for active pharmaceutical
ingredients,
has a wide range of particle and pore morphology. A thorough understanding
of ingredients used in MPS synthesis is an important prerequisite
for optimizing its physicochemical characteristics. The present study
aimed to evaluate the effect of glycerol and hydrochloric acid on
the characteristics of synthesized MPS. Ordered MPS materials were
synthesized using the pluronic P123 template and tetraethyl orthosilicate
(TEOS) precursor. A three-level factorial design was employed to study
the interaction between glycerol and hydrochloric acid. The optimized
MPS particles were reasonably uniform in shape (short and rod-shaped)
and < 1 μm in size with a smooth surface morphology. The
nitrogen adsorption–desorption analysis revealed that the uniform
cylindrical pores of the prepared MPS had a diameter > 5 nm and
a
total surface area > 500 m
2
/g. With increasing acid
and
glycerol concentrations, the particle size of MPS decreased. However,
while the glycerol increased the heterogeneity of the synthesized
particles, the acid decreased it. The developed MPS was successfully
loaded with a biological drug (insulin) with a 21.94% encapsulation
efficiency. The MPS prepared in this study exhibits potential applications
as a drug delivery carrier for drugs with a large molecular weight.
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