Different trends for preparation of budesonide pellets with enhanced dissolution rate

The current research attempts different approaches to overcome the poor dissolution of budesonide (a poorly water-soluble drug) from pellet formulations. Various methods such as liqui-pellet (LP) and pellets made of solid dispersion (SDP) were employed and compared to conventional pellets (CP). In SDP method, budesonide:PVP solid dispersion was prepared followed by extrusion-pelletization. Solid dispersion of budesonide-PVP was also layered to the surface of placebo pellets (LSDP). In LP technique, budesonide dispersed in PEG 400 was mixed with Avicel or Avicel:lactose and was extruded-spheronized. Pellets were evaluated for their shape, size, mechanical properties and dissolution rate. The pellets made by LSDP method were significantly harder than CP or PSDP. LP with a loading factor greater than 0.34 was very soft compared to CP and SDP. Pelletization of budesonide SD (PSDP) did not have a tremendous effect on the dissolution enhancement of budesonide compared to CP whilst LSDP showed faster drug release. In conclusion, the layering of budesonide solid dispersion on placebo pellets (LSDP) was the most promising approach for the production of pellets with the highest dissolution rate so that more than 80% of the drug was released within the first 5 min. Also this formulation had proper mechanical properties. This method has the capability to overcome the poor dissolution of budesonide associated with the pellet containing Avicel, and could be employed for the dissolution enhancement of other poorly water-soluble drugs in pellet form.     

Formulation optimization of controlled-release pellets of metoclopramide hydrochloride using dissolution fit factor approach

The purpose of this study was to optimize the formulation variables for the preparation of ethyl cellulose-coated nonpareils loaded with metoclopramide hydrochloride (MCL). The approach to evaluate the effectiveness of formulation parameters was monitored by release rate testing using dissolution fit factors as a tool. The content of ethyl cellulose used in the formulation was based on the drug-loaded weight. The interrelationship of each developed formulation and the reference formulation Gastro-Timelets and their respective dissolution curves were evaluated using Moore's equation: [equation: see text]. The relationship between the ethyl cellulose content in the formulation and the dissolution fit factor f2 can be described as the following regression equation: Y = -0.054X2 + 3.347X - 1.915 (r2 = 0.99). The optimum ethyl cellulose content obtained from the equation was 30.8%. The type and content of plasticizer used in the formulation to achieve the greatest f2 were determined to be Myvacet 9-40 at the concentration of 25%. Results indicated that using the release rate testing approach with the dissolution fit factor as a tool could provide valuable information for formulation optimization.     

Development of a tamsulosin hydrochloride controlled-release capsule consisting of two different coated pellets

Tamsulosin hydrochloride (TSH) controlled-release capsule (pellets) was successfully prepared using a novel, simple, and flexible multiunit drug delivery system, which consisted of two different coated pellets. The TSH-loaded core pellets consisting of microcrystalline cellulose (MCC), lactose, Carbopol(R) 974P, and the active agent, were prepared by extrusion/spheronization method. Eudragit NE30D and Eudragit L30D-55 were used as the coating materials to prepare sustained-release (SR) pellets and enteric-release (ER) pellets. The coated pellets were prepared using two different equipments: centrifugal coater and fluidized-bed coater. By adjusting the ratio of SR and ER pellets, more than one blend ratios, which meet the in vitro release criterion were obtained. A similarity factor (f(2)) was employed to choose the optimum proportion compared with the commercial product (Harnal capsule). The morphology of the pellet surfaces was examined by scanning electron microscopy (SEM) before and after dissolution. The release profiles were significantly affected by changing the proportions of SR and ER. The optimum ratio is SR:ER = 2:1 using a centrifugal coater (f(2) = 61.93) and SR:ER = 3:1 using a fluidized coater (f(2) = 66.42). This result suggests that blending these two-part pellets (SR and ER) can provide an alternative to preparing a controlled-release dosage form, instead of blending of the coating polymer.     

Controlled-release behavior of diphenhydramine hydrochloride loaded neutral microgranules and coated using ethylcellulose water dispersion

The development of a loading method of a water-soluble drug using aqueous binding solution to produce microgranules that were then coated with an aqueous ethylcellulose dispersion to sustain drug release is described. The results, in terms of drug used, showed that besides the fluidized bed parameters, the amount of drug dissolved in the binder solution plays an important role in obtaining a satisfying result during the spraying process. Thus, it seems necessary to determine the critical concentration above which the material started to adhere to the interior of the fluidization column, and the possibility of drug layering onto carrier material is aggravated. ANOVA of the time parameter for release of 63.2% of total drug (td) value showed significant influence of ethylcellulose (Aquacoat ECD-30) and dibutyl sebacate concentration on diphenhydramine hydrochloride (DPH) release. The dissolution rate decreased with an increase in polymer concentration. The diffusional exponent n of the Peppas equation indicated that the DPH release kinetic was non-Fickian but approached Fickian diffusion, particularly at higher coating levels.     

Electrostatic fields of an infinite medium containing arbitrarily positioned coated cylinders

We propose a framework for evaluation of the electrostatic fields in an unbounded isotropic medium containing a number of arbitrarily dispersed circular cylinders or coated cylinders subjected to a remotely prescribed potential field. The cylinders or coated cylinders could be at most cylindrically orthotropic, and may have different radii with different conductivities. The approach is based on a multipole expansion formalism, together with a construction of consistency conditions and translation operators. This main procedure is inspired from an ingenious concept of the classic work of Lord Rayleigh [1], in which the effective conductivity of a periodic array of circular disks or spheres is considered. In the present formulation, we expand the potential field versus various local coordinates with origins positioned at the inclusions’ centers. The key step is to link the potential data with the outer applied field, which is accomplished by the use of Green’s second identity in the matrix domain. We show that the coefficients of field expansions are governed by an infinite set of linear algebraic equations. Numerical results are presented for a few different configurations. We have verified our numerical solutions for a simplified configuration with those obtained from the bipolar coordinate transformation.     

Mechanistic analysis of drug release from theophylline pellets coated by films containing pectin, chitosan and Eudragit RS

The objective of this study was to obtain detailed information on the mechanism of drug release from mixed-film of pectin-chitosan/Eudragit® RS. Pellets (710-840 μm in diameter) containing 60% theophylline and 40% microcrystalline cellulose were prepared by extrusion-spheronization method. Eudragit® L100-55 enteric coating capsules included film-coated pellets of theophylline in theoretical coating weight gains of 10, 15, and 20%, with pectin-chitosan complex contents of 5, 10, 15, and 20% for each level of weight gain were prepared and subjected to in vitro drug release. Drug release from this system showed a bimodal release profile characteristic with the drug release enhancement, being triggered (burst release) in the colonic medium. The reason for burst drug release may be due to the enzymatic degradation of pectin via pectinolytic enzymes in the simulated colonic medium. The mechanism of drug release from each formulation was evaluated in the terms of zero-order, first-order, Higuchi and Korsmeyer-Peppas models. It was observed that none of the enteric coating capsules showed any drug release in the simulated gastric medium (phase I). The analysis of release profiles showed that zero-order kinetics was found as the better fitting model for all formulations in the simulated small intestine (phase II) and it could be due to the pectin-chitosan swelling and subsequent formation of aqueous channels. In the colonic medium (phase III), due to degradation of pectin and its leaching from the mixed-film, there was a modification in drug release kinetics from swelling-controlled at phase II to anomalous at phase III. It also was found that both zero-order and Higuchi models contributed in colonic drug release from most of the formulations.     

Influence of Eudragit NE 30 D blended with Eudragit L 30 D-55 on the release of phenylpropanolamine hydrochloride from coated pellets

The objective of this study was to investigate the influence of Eudragit® NE 30 D blended with Eudragit® L 30 D-55 on the release of phenylpropanolamine hydrochloride (PPA·HCl) from coated pellets. The miscibility of Eudragit NE 30 D/L 30 D-55 blends at different ratios was studied by using differential scanning calorimetry. The release of PPA·HCl from pellets coated with Eudragit NE 30 D alone and a Eudragit NE 30 D/L 30 D-55 blend, when stored at 40°C and 60°C, was determined by UV spectroscopy. Eudragit NE 30 D and Eudragit L 30 D-55 were miscible in ratios greater than 4:1. The curing time that was required to reach an equilibrium state decreased with the addition of Eudragit L 30 D-55. The presence of Eudragit L 30 D-55 also produced a film coating that was less tacky, and a dispersion of Eudragit NE 30 D containing Eudragit L 30 D-55 (5:1) was shown to prevent agglomeration of the pellets during coating and storage.     

Insights into the dissolution mechanisms of detergent agglomerates: An approach to assess dissolution heterogeneity

In this work, the dissolution mechanisms of detergent agglomerates with different binders were investigated in aqueous solution. The dissolution processes of detergent agglomerates were online monitored by using in situ UV–VIS spectrophotometer and electric conductivity probe. Dissolution profiles were correlated by Weibull model to evaluate the time-dependent dissolution rate coefficient and to classify the type of dissolution rate function k_t(t). The Kullback-Leibler information distance d_K-L was proposed to assess the degree of dissolution heterogeneity. The results indicate that the sodium linear alkylbenzene sulfonates (NaLAS) and sodium carbonates (Na₂CO₃) in detergent agglomerates have different dissolution behaviors, and their dissolution rates are influenced by the type and content of binders. Moreover, detergent agglomerates using semi-solid NaLAS paste or liquid linear alkylbenzene sulfonic acid (HLAS) as binders in granulation processes follow different dissolution mechanisms in water.     

Assessment of the multi-compound non-equilibrium dissolution behaviour of a coal tar containing PAHs and phenols into water

Herein, an experimental study coupled with a model in order to assess the non-equilibrium and multi-compound dissolution behaviour of a coal tar containing PAHs and phenols into water, is presented. For this aim, two experimental studies has been carried out: (1) coal tar-water partition equilibrium and (2) dissolution dynamics of coal tar under controlled hydrodynamic conditions in percolation columns packed with glass beads. The dissolution amount of the three target constituents (i.e. phenol, naphthalene and phenanthrene) was monitored by UV detection. The dissolution behaviour was modelled using a predictive fraction approach. The partition coefficients have been estimated from experimental data and the obtained results show that the partition coefficient of each constituent between the aqueous phase and the tar depends on the activities of the constituent in both phases and cannot be estimated only from the solubility of the pure compound in water. The non-equilibrium dissolution model was established, applied for the experimental conditions and validated for three target compounds adjusting the effective interfacial area between tar and water. This parameter is specific of the experimental set-up. The global behaviour of coal tar has been modelled taking into account four categories of compounds according to their water solubility and volatilities. The mass transfer parameters have been estimated using available correlations. The results of this paper indicate that a model based on component fractions can be used to assess the non-equilibrium dissolution behaviour of a coal tar.     

The MiniWiD-COATER: II. Comparison of acid resistance of enteric-coated bisacodyl pellets coated with different polymers

Neutral pellets were loaded with bisacodyl and enteric-coated with hydroxypropyl methylcellulose acetate succinate (HPMCAS), carboxymethyl ethylcellulose (CMEC), cellulose acetate trimellitate (CAT), and poly(ethylacrylate, methacrylic acid) (Eudragit L 30 D) in a miniature fluid-bed pan coater called MiniWiD. Gastric juice resistance was tested by dissolution using USP Apparatus 2 (paddle) in 0.1 N hydrochloric acid under sink conditions over 6 hours. As a measure of enteric coating quality the USP specifications were used meaning that no more than 10 % of the drug should be released within 2 hours.

Organic-solvent based films of HPMCAS, CMEC and CAT at a coating level of 18 to 25 % provided gastroresistance for more than 6 hours. Aqueous suspensions of HPMCAS and CMEC as well as the ammonium salt aqueous solutions of CAT produced films with a short gastroresistance of below 0.6 hours. By doubling the coating level of water-based HPMCSD films the protection was prolonged to 3.4 h.

Enteric coatings were obtained from all aqueous latex dispersions of Eudragit L 30 D at a coating level of 24 %. The alteration of coating temperature between 25 and 45 °C had no significant effect on the release rates, whereas the variation of type and amount of plasticizer led to a different release rate after 2 hours. Best protection was obtained using films plasticized with 20 % of dibutyl phthalate (DBP) allowing a release of only 4 % of the drug in 6 hours although the application temperature was 15 °C below the minimum film-forming temperature (MFT). All coatings dissolved in artificial intestinal fluid within 15 minutes.     

The MiniWiD-COATER: II. Comparison of acid resistance of enteric-coated bisacodyl pellets coated with different polymers

Abstract

Neutral pellets were loaded with bisacodyl and enteric-coated with hydroxypropyl methylcellulose acetate succinate (HPMCAS), carboxymethyl ethylcellulose (CMEC), cellulose acetate trimellitate (CAT), and poly(ethylacrylate, methacrylic acid) (Eudragit L 30 D) in a miniature fluid-bed pan coater called MiniWiD. Gastric juice resistance was tested by dissolution using USP Apparatus 2 (paddle) in 0.1 N hydrochloric acid under sink conditions over 6 hours. As a measure of enteric coating quality the USP specifications were used meaning that no more than 10 % of the drug should be released within 2 hours.

Organic-solvent based films of HPMCAS, CMEC and CAT at a coating level of 18 to 25 % provided gastroresistance for more than 6 hours. Aqueous suspensions of HPMCAS and CMEC as well as the ammonium salt aqueous solutions of CAT produced films with a short gastroresistance of below 0.6 hours. By doubling the coating level of water-based HPMCSD films the protection was prolonged to 3.4 h.

Enteric coatings were obtained from all aqueous latex dispersions of Eudragit L 30 D at a coating level of 24 %. The alteration of coating temperature between 25 and 45 °C had no significant effect on the release rates, whereas the variation of type and amount of plasticizer led to a different release rate after 2 hours. Best protection was obtained using films plasticized with 20 % of dibutyl phthalate (DBP) allowing a release of only 4 % of the drug in 6 hours although the application temperature was 15 °C below the minimum film-forming temperature (MFT). All coatings dissolved in artificial intestinal fluid within 15 minutes.     

Electroluminescence: enhanced injection using ITO electrodes coated with a self assembled monolayer

In a typical organic bilayer electroluminescent device the hole injecting electrode is almost invariably ITO glass, but a number of electron injecting metal electrodes are possible. Unfortunately the low work function materials used readily oxidise and restrict the lifetime of the device. It is known that appropriate monolayers can change the work function of a solid and also that phosphonic acids can form self assembled monolayers on ITO glass. Using an ITO glass electrode coated with a self assembled monolayer of an electron accepting phosphonic acid (2-chloroethanephosphonic acid) and aluminium as the electron injecting electrode, it was found that the threshold voltage was significantly reduced to the same value as achieved with the less stable Mg:Ag electrode. The use of such modified ITO electrodes would obviate the use of highly reactive metal electrodes and help to overcome one of the factors which limit device lifetime.     

Controlled precipitation for enhanced dissolution rate of flurbiprofen: development of rapidly disintegrating tablets

Objective: The aim of this work was to investigate the potential of controlled precipitation of flurbiprofen on solid surface, in the presence or absence of hydrophilic polymers, as a tool for enhanced dissolution rate of the drug. The work was extended to develop rapidly disintegrated tablets.

Significance: This strategy provides simple technique for dissolution enhancement of slowly dissolving drugs with high scaling up potential.

Methods: Aerosil was dispersed in ethanolic solution of flurbiprofen in the presence and absence of hydrophilic polymers. Acidified water was added as antisolvent to produce controlled precipitation. The resultant particles were centrifuged and dried at ambient temperature before monitoring the dissolution pattern. The particles were also subjected to FTIR spectroscopic, X-ray diffraction and thermal analyses.

Results: The FTIR spectroscopy excluded any interaction between flurbiprofen and excipients. The thermal analysis reflected possible change in the crystalline structure and or crystal size of the drug after controlled precipitation in the presence of hydrophilic polymers. This was further confirmed by X-ray diffraction. The modulation in the crystalline structure and size was associated with a significant enhancement in the dissolution rate of flurbiprofen. Optimum formulations were successfully formulated as rapidly disintegrating tablet with subsequent fast dissolution.

Conclusions: Precipitation on a large solid surface area is a promising strategy for enhanced dissolution rate with the presence of hydrophilic polymers during precipitation process improving the efficiency.     

Co-crystallization for enhanced dissolution rate of bicalutamide: preparation and evaluation of rapidly disintegrating tablets

Objectives: Enhance the dissolution rate of bicalutamide via co-crystallization with sucralose (sweetener), with the aim to develop rapidly disintegrating tablets with subsequent prompt dissolution.

Significance: Bicalutamide is antiandrogenic agent for the treatment of prostate cancer but has low and variable oral bioavailability, mainly attributed to poor dissolution. Co-crystallization with benign excipients is promising for dissolution enhancement with the additive serving dual functions. The benefit will become greater if dissolution enhancement is associated with the development of orodispersible tablets which is suitable for elderly patients who are the most vulnerable for prostate cancer.

Methods: Bicalutamide was dissolved in acetone in the presence of increasing molar ratios of sucralose. The solvent was evaporated while mixing to deposit crystals that were subjected to wet co-grinding until drying. The developed solids were characterized using Fourier transform infrared spectroscopy, differential thermal analysis and X-ray diffraction in addition to monitoring bicalutamide dissolution.

Results: Instrumental analysis provided evidences for co-crystallization which was initiated at 1:1 molar ratio of bicalutamide to sucralose with complete co-crystallization at 1:4 molar ratio. The co-crystals provided faster bicalutamide dissolution compared with the unprocessed drug and that recrystalized from acetone in the absence of sucralose. The formulation containing bicalutamide with sucralose at 1:4 molar ratio was selected for tablet formulation into which superdisintegrants were included. The developed tablets exhibited flash disintegration with subsequent fast dissolution of bicalutamide.

Conclusions: The study introduced co-crystallization of bicalutamide with sucralose as an efficient tool to enhance the dissolution rate and to develop rapidly dissolving tablets for intraoral administration.     

Solid dispersion adsorbate technique for improved dissolution and flow properties of lurasidone hydrochloride: characterization using 32 factorial design

The aim of the present study was to improve the dissolution and flow properties of lurasidone hydrochloride (LH) by solid dispersion adsorbate (SDA) technique. Solid dispersions (SDs) of LH were prepared by fusion method using Poloxamer P188. The melt dispersion was adsorbed onto the porous carrier Florite (calcium silicate). A 3² factorial design was employed to quantify the effect of two independent variables, namely ratio of carrier (Poloxamer 188) and LH in SD and ratio of adsorbent (Florite) to SD. SDA granules of LH were studied for flow properties and characterized using differential scanning calorimetry, scanning electron microscopy, and X-ray diffraction. Tablets of optimized composition of SDA granules (equivalent to 20?mg of drug) and plain tablets were prepared by direct compression method. The dissolution studies were carried out in Mcllvaine buffer (pH 3.8) as per USFDA guidelines and characterized for parameters such as percent dissolution efficiency, t₅₀, and Q₃₀. Tablets prepared from SDA granules showed almost four-fold increase in cumulative percentage drug release as compared to tablets prepared from plain LH. The value of dissolution efficiency was enhanced from 49.60% for plain tablets to 94.15% for SDA tablets. SDA granules did not show any change in drug release and X-ray diffraction pattern after storage at 40?°C/75% of RH for 3?months, which confirms that Florite prevented conversion of drug from amorphous form to crystalline form improving physical stability of the amorphous state of LH.     

Development of controlled-release buccoadhesive hydrophilic matrices of diltiazem hydrochloride: optimization of bioadhesion,dissolution, and diffusion parameters

Buccoadhesives have long been employed to improve the bioavailability of drugs undergoing significant hepatic first-pass metabolism. Diltiazem hydrochloride (DLZ) is also reported to have low oral bioavailability due to an extensive hepatic first-pass effect. Controlled-release buccoadhesive hydrophilic matrices containing DLZ were prepared using a 3(2) factorial design. Amounts of Carbopol 934P (CP) and Methocel K100LV (HPMC) were taken as the formulation variables (factors) for optimizing bioadhesion, and kinetics of dissolution and diffusion. A mathematical model was generated for each response parameter. Bioadhesive strength tended to vary quite linearly in increasing order with increasing amount of each polymer. The drug release pattern for all the formulation combinations was found to be non-fickian, approaching zero-order kinetics. The values of permeation coefficient tended to vary non-linearly with polymer amount, depicting the plausibility of interaction between the two polymers. Suitable combinations of the two polymers provided adequate bioadhesive strength and a fairly regulated release profile up to 10 hr. The response surfaces and contour plots for each response parameter are presented for further interpretation of the results. The optimum formulations were chosen and their predicted results found to be in close agreement with experimental findings.     

Proliposome powders for enhanced intestinal absorption and bioavailability of raloxifene hydrochloride: effect of surface charge

The primary goal of the present study was to investigate the combined prospective of proliposomes and surface charge for the improved oral delivery of raloxifene hydrochloride (RXH). Keeping this objective, the present systematic study was focused to formulate proliposomes by varying the ratio of hydrogenated soyphosphatidylcholine and cholesterol. Furthermore, to assess the role of surface charge on improved absorption of RXH, anionic and cationic vesicles were prepared using dicetyl phosphate and stearylamine, respectively. The formulations were characterized for size, zeta potential and entrapment efficiency. The improved dissolution characteristics assessed from dissolution efficiency, mean dissolution rate were higher for proliposome formulations. The solid state characterization studies indicate the transformation of native crystalline form of the drug to amorphous and/or molecular state. The higher effective permeability coefficient and fraction absorbed in humans extrapolated from in situ single-pass intestinal absorption study data in rats provide an insight on the potential of proliposomes and cationic surface charge for augment in absorption across gastro intestinal barrier. To draw the conclusions, in vivo pharmacokinetic study carried out in rats indicate a threefold enhancement in the rate and extent of absorption of RXH from cationic proliposome formulation which unfurl the potential of proliposomes and role of cationic charge for improved oral delivery of RXH.     

Drug release from spray layered and coated drug-containing beads: effects of pH and comparison of different dissolution methods.

Based on dissolution profiles of three model drugs on spray layered beads with the same percentage of Aquacoat coating, it was concluded that in vitro dissolution of oral controlled-release formulations should be performed in both gastric and intestinal media for ionizable drugs. Ketoprofen (weak acid, pKa 4.8), nicardipine HCl (salt of weak organic base, pKa 8.6), and acetaminophen (very weak organic acid, pKa 9.7, not ionized at physiologic pH) provided different dissolution characteristics in enzyme-free simulated gastric fluid (pH 1.4) and enzyme-free simulated intestinal fluid (pH 7.4), indicating that the rate of drug release was pH dependent and related to drug ionization even though the solubility of the coating (ethylcellulose) is pH independent. In acidic media, ketoprofen release from the beads containing low-level coating (3%) was slower than that of nicardipine HCl, with the opposite holding true in basic media. Acetaminophen was released at approximately the same rate in both acidic and basic media. A comparison of drug release profiles for nicardipine HCl nude beads was also investigated among three different dissolution methods: USP dissolution apparatus I (basket method, 50 rpm), USP dissolution apparatus II (paddle method, 50 rpm), and USP dissolution apparatus III (Bio-Dis, Van-Kel Industries, 5 and 10 dpm). Release profiles obtained from all methods were similar, indicating that the three dissolution methods were comparable.     

Film Coated Pellets Containing Verapamil Hydrochloride: Enhanced Dissolution into Neutral Medium

Abstract

Weakly basic drugs, such as verapamil hydrochloride, that are poorly soluble in neutral/alkaline medium may have poor oral bioavailability due to reduced solubility in the small intestine and colon. Film coated pellets were prepared using two strategies to enhance drug release at high pH values. Firstly, pellets were coated with Eudragit® RS/hydroxypropyl methylcellulose acetate succinate (HMAS) mixtures in proportions of 10:1 and 10:3, respectively. The enteric polymer, HMAS, would dissolve in medium at pH>6 creating pores through the insoluble Eudragit RS membrane to increase drug release. Secondly, an acidic environment was created within the core by the inclusion of fumaric acid at concentrations of 5 and 10% in order to increase drug solubility. Both strategies enhanced drug release into neutral medium in dissolution studies using the pH change method to simulate GIT transit. Dissolution profiles of samples tested in pH 1.2 for 12 hr were compared with those using the pH change method (pH 1.2 for first 1.5 hr, pH raised to 6.8 for remaining 10.5 hr) using the area under the dissolution curve (AUC), the dissolution half-life (t_50%), and the amount of drug released in 3 hr (A_{3 hr}) values. Both strategies enhanced drug release into neutral medium although the strategy using HMAS in the film was more effective. The formulation least affected by pH change was a combination of the two strategies, i.e., pellets containing 5% fumaric acid coated with Eudragit RS 12% w/w and HMAS 1.2% w/w.     

Insights into Electrolytic Pre-Lithiation: A Thorough Analysis Using Silicon Thin Film Anodes

Pre-lithiation via electrolysis, herein defined as electrolytic pre-lithiation, using cost-efficient electrolytes based on lithium chloride (LiCl), is successfully demonstrated as a proof-of-concept for enabling lithium-ion battery full-cells with high silicon content negative electrodes. An electrolyte for pre-lithiation based on γ-butyrolactone and LiCl is optimized using boron-containing additives (lithium bis(oxalato)borate, lithium difluoro(oxalate)borate) and CO₂ with respect to the formation of a protective solid electrolyte interphase (SEI) on silicon thin films as model electrodes. Reversible lithiation in Si||Li metal cells is demonstrated with Coulombic efficiencies (C_Eff) of 95–96% for optimized electrolytes comparable to 1 m LiPF₆/EC:EMC 3:7. Formation of an effective SEI is shown by cyclic voltammetry and X-ray photoelectron spectroscopy (XPS). electrolytic pre-lithiation experiments show that notable amounts of the gaseous product Cl₂ dissolve in the electrolyte leading to a self-discharge Cl₂/Cl⁻ shuttle mechanism between the electrodes lowering pre-lithiation efficiency and causing current collector corrosion. However, no significant degradation of the Si active material and the SEI due to contact with elemental chlorine is found by SEM, impedance, and XPS. In NCM111||Si full-cells, the capacity retention in the 100th cycle can be significantly increased from 54% to 78% by electrolytic pre-lithiation, compared to reference cells without pre-lithiation of Si.