Optimization of entrapment efficiency and release of clindamycin in microsponge based gel

The aim of the present study was to formulate clindamycin (CLN) as a microsponge based gel to release the drug in a controlled manner and reduce the side effects in the treatment of acne. Since this method requires poor water solubility of the drug to be loaded in particles, therefore, conversion of the hydrochloride salt to free base was done. By using an emulsion solvent diffusion method, we made six different formulations of microsponges containing CLN-free base by changing the proportions of polymer, emulsifier and the pH of the external phase. These formulations were studied for physical characterization and for drug- polymer interactions. The physical characterization showed that microsponge formulations coded by C5, C6 resulted in a better loading efficiency and production yield and their particle size was less than 30 µm. Scanning electron microscopy images showed the microsponges porous and spherical. C5, C6 microsponge formulation was prepared as gel in Carbopol and in vitro evaluated. The microsponge formulation gel C8 was found to be optimized. C8 released 90.38% of drug over 12 h and showed viscosity 20,157 ± 38 cp, pH of 6.3 ± 0.09 and drug content of 99.64 ± 0.04%. Fourier transform infrared spectroscopy and differential scanning calorimetry confirmed no significant interactions between excipients and drug.

FORMULATION AND EVALUATION OF GLICLAZIDE NANOSPONGES

Objective: The objective of the present study was to develop and characterize an optimal stable nanosponges of Gliclazide (GLZ) by using the emulsion solvent diffusion method and aimed to increase its bioavailability and release the drug in sustained and controlled manner. Methods: The GLZ nanosponge was prepared by emulsion solvent diffusion method using different drug-polymer ratios (1:1 to 1:5) Eudragit S100 is used as a polymer. Differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR) estimated the compatibility of GLZ with polymer. All formulations evaluated for production yield, entrapment efficiency, in vitro drug release, scanning electron microscopy (SEM) and stability studies. Results: The DSC and FTIR Studies revealed that no interaction between drug and polymer. The Production yield of all batches in the range of 73.8±0.30 to 85.6±0.32. Batch F3 showed the highest production yield, the entrapment efficiency of batch F3 70.6±0.77. The average particle size ranges from 303±2.36 to 680±2.50 nm. By the end of 10th hour F3 formulation shown highest drug release was found to be 94.40±1.12%. The release kinetics of the optimized formulation shows zero-order drug release. The stability study indicates no significant change in the in vitro dissolution profile of optimized formulation. Conclusion: The results of various evaluation parameters, revealed that GLZ nanosponges would be possible alternative delivery systems to conventional formulation to improve its bioavailability, the emulsion solvent diffusion method is best method for preparation of nanosponges and release the drug in sustained and controlled manner.

Formulation and Evaluation of Copper Nanoparticles Loaded Microsponges

Microsponges become imperative in the field of targeted drug delivery and in other biomedical applications. There was a clamant need for designing microsponges incorporating with green synthesised metal nanoparticles rather than the chemical drug in order to reduce the side effects of the drug and thus increasing the effectiveness of nature of the whole material. It provokes us to design this novel approach of loading copper nanoparticles into the microsponges. Here in this work, microsponges based on ethyl cellulose and polyvinyl alcohol were synthesised by Quasi-Emulsion Solvent diffusion method in which copper nanoparticles procured from Hibiscus rosa-sinensis leaf extract was incorporated. The Loaded microsponges were characterised by High Resolution Scanning Electron Microscopy (HR-SEM) and Particle size distribution Analyzer (PSA). The Drug content and Entrapment Efficiency of the microsponges were found out. The antimicrobial and antioxidant activity of the loaded microsponges were evaluated.

Studying the effect of variables on baclofen floating microsponge

The aim of the present work was to develop a microsponge delivery system of baclofen to control its release and thereby reducing dosing frequency and enhancing patient compliance. The microsponge was produced by oil in oil emulsion solvent diffusion method. The effects of drug/polymer ratio, stirring time and type of Eudragit polymer on the physical characteristics of microsponges were investigated. The prepared microsponges was characterized for production yield (PY), loading efficiency (LD), particle size, surface morphology, and in vitro drug release. The results showed that the microsponge formula with Eudragit RS100 had optimum physical properties with PY % equal to 97 %, and LD % equal to 81% and controlled drug release (75% of drug release in 8 hours) when compared with other formulas and pure BFN. Therefore, the non-‎aqueous emulsion solvent diffusion method is a promising method to produce baclofen microsponges.‎

PREPARATION AND EVALUATION OF PARECOXIB MICROSPONGE HYDROGEL SUSTAINED RELEASED TABLET

Microsponges are the polymeric drug delivery systems composed of porous microspheres. They are tiny sponge like spherical particles that consists of myriad of inter-connecting voids within a non-collapsible structure with a large porous surface. The present work is to formulate and evaluate the Parecoxib Microsponge Hydrogel Sustained Release Tablet. The Microsponges of Parecoxib is prepared by Quasi-emulsion solvent diffusion method using Ethyl cellulose and Eudragit RS100 as polymers and Di-butyl phthalate as Plasticizer. And they are characterized for FTIR studies, production yield, particle size analysis, DSC and SEM. The production yield of formulations was from 77.77 to 82.75. FTIR and DSC studies are revealed that the drug and polymer are compatible with each other during preparation. The average diameter of Microsponge is ranged from 536.9 nm to 489.7. Parecoxib Microsponge hydrogel were prepared as sustained release tablets by using sustained release polymers like MCC, Magnesium stearate, Lactose and talc. Preformulation of Microsponge granules were carried out by various parameters and post formulation were carried out by In-vitro dissolution studies, hardness, friability and weight variation tests. Formulation F3 shows good results for the drug release kinetics as controlled release and F6 formulation shows good results for the in-vitro dissolution studies for sustained release. Key words: Microsponge hydrogel drug delivery, Parecoxib, Sustained drug release tablets, quasi emulsion solvent diffusion method.

Preparation and Characterization of Etodolac as a Topical Nanosponges Hydrogel

Nanosponges (NS) of etodolac(ETO) was prepared using the emulsion solvent diffusion method ; the effects of drug: polymer ratio, the effect of level concentration of internal phase and stirring time and other variables that effect on the physical characteristics of NS were investigated and characterized, The selected formula was lyophilized then incorporated into hydrogel ; which also evaluated .The results show that the formulation that contain Drug: PVA:EC in ratio 1:3:2 is the best with smallest particle size 40.2±0.098 with polydispersibility0.005 and in vitro release 97.6±0.11%, , ETO NS Carbopol hydrogel produced a significant(p<0.05) improvement of the in vitro release than pure ETO hydrogel.

The NANOSPONGES: AN INNOVATIVE DRUG DELIVERY SYSTEM

For prolonged time there is a delusion for efficacious targeted drug delivery system, but the chemistry hold complex form had made situations thorny, but the development of new colloidal carrier called nanosponges (NSs) likely circumvent these problems. NSs are the nanoporous particles that can entangle a huge range of material and then be engulfed into a suitable formulation depend on the route of administration. They prevent the drug-protein degradation, lengthen the drug release in a controlled manner, and release the medicament to the target site. They can travel around the body and attach on the surface and liberate the drug in a controlled and predictable manner at the specific target site. They are fine aqueous solubility which makes them a bearer for low water-soluble drugs. Drugs having low bioavailability are best suited for this type of carrier system. Both lipophilic and hydrophilic drugs can be included in NSs. Particle size can change from smaller to bigger by varying the amount of crosslinker to the polymer. Various applications of NSs such as recovering bioavailability of active ingredient molecule and delivery of active ingredient into oral, topical, parenteral, and nasal route make them a superior candidate for targeted delivery of drugs. It can be used as a shipper for biocatalysts in the transport and release of enzymes, proteins, vaccines, and antibodies. They can be prepared by different methods such as emulsion solvent diffusion method, melt method, ultrasound-assisted method, Quasi emulsion solvent diffusion method. This analysis is focusing on the advantages, formulation, evaluation, application, and patent report of the NSs.

Human Hair Keratin Microspheres Prepared by the Water-In-Oil Emulsion Solvent Diffusion Method for Hydrophilic Drug Carrier

Human hair keratin (HK) was prepared with reducing agent and used in solution to construct microspheres by the simple emulsion solvent diffusion method. The obtained microspheres were observing under scanning electron microscope (SEM). The shape, size distribution and content of microspheres were influenced by W:O ratios. A and 1% w/v keratin solution and 100 mL of oil phase were optimal conditions for fabrication of HK microspheres. The authors studied drug loading efficiency of the HK microspheres by using blue-dextran a model drug and found that the drug loading efficiency as well as releasing profile of blue-dextran were gradually increased by increasing keratin concentration. In conclusion, HK microspheres could be used as hydrophilic carrier molecules for drug delivery system application.

In Vitro and In Vivo Evaluation of Desogestrel-Loaded Poly(D,L-lactic Acid) Nanoparticles

The aim of this study was to explore the synthesis parameters of desogestrel-polylactic acid nanoparticles (DG-PLA-NPs), optimise the preparation technology, and elucidate the in vitro release characteristics. Considering encapsulation efficiency (EE) and drug loading as the main evaluation indexes, DG-PLA-NPs were prepared using the modified emulsion solvent diffusion method and single factor and orthogonal design tests were performed to investigate the influencing factors and optimise the preparation method. Morphology of the nanoparticles was observed using transmission electron microscopy (TEM), average particle diameter and distribution were determined using dynamic laser particle size analysis, and the EE and drug loading were measured using reversed-phase high-performance liquid chromatography. Among the eight factors, the drug-to-material ratio, water-to-organic phase ratio, and polyvinyl alcohol (PVA) concentration significantly affected the NP EE. In the optimised formulation, the PLA/DG ratio, PVA concentration, and oil-to-water phase ratio were 5, 0.5%, and 5, respectively. The DG-PLA-NPs prepared with the optimised formulation were round or spherical with an average diameter of 209 nm, 79.60% EE, and 6.81% drug loading capacity. The polydispersity index was 0.181, and the zeta potential was −27.37 mV. The in vitro releases of both DG and DG-PLA-NPs conformed to the Weibull equation. The DG-PLA-NPs released desogestrel rapidly in the early stages but slowly at later stages, indicating that compared to DG, the DG-PLA-NPs had obvious sustained-release effects. The DG-PLA-NPs prepared by the modified emulsion solvent diffusion method were small, simple to prepare, and had high drug loading with promising application prospects.

Studying the effect of variables on Acyclovir microsponge

The aim of the present investigation was to develop a microsponge delivery system of acyclovir to control its release when applied topically thereby reducing dosing frequency and enhancement patient compliance. The microsponges were produced by the oil in oil emulsion solvent diffusion method. The effect of different formulation and process variables such as internal phase volume, polymer type, drug-polymer ratio, stirring speed and stirring duration on microsponge production yield, loading efficiency, particle size and in-vitro drug release was evaluated. The result showed that the microsponge F2 prepared from Eudrajet RS polymer had optimum physical properties regarding the loading efficiency of 99.71_+ 0.7% and production yield which was 85%. Also, F2 showed 66% drug release within 8 hours. Accordingly, the oil in oil emulsion solvent diffusion method is an effective technique to formulate microsponges with maximum production yield and loading efficiency for acyclovir.